GSK3326595
Quick Overview for GSK3326595 (ABIN7233257)
应用范围
Chemical Name
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原理
- Selective PRMT5 inhibitor
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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.
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纯度
- >98 %
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Formula
- C24H32N6O3
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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
Anacardic AcidInh 16611-84-0 2-Hydroxy-6-pentadecylbenzoic acid
EX-527Inh Cell-permeable 49843-98-3 6-chloro-2,3,4,9-tetrahydro-1H-carbazole-1-xarboxamide (racemic)
ResveratrolAct 501-36-0 3,4',5-Trihydroxy-trans-stilbene
5-AzacytidineInh Cell-permeable 320-67-2 4-Amino-1-ß-D-ribofuranosyl-1,3,5-triazin-2(1H)-one
NicotinamideInh 98-92-0 Pyridine-3-carboxylic acid amide
AS-8351Inh 796-42-9 2-Hydroxy-1-naphthylaldehyde isonicotinolyhydrazone
UNC-0379Inh 1620401-82-2 6,7-Dimethoxy-2-(pyrrolidin-1-yl)-N-(5-(pyrrolidin-1-yl)-pentyl)quinazolin-4-amine
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限制
- 仅限研究用
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状态
- Powder
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储存条件
- -20 °C
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背景
- EPZ015938,Proliferation,Epigenetics,Posttranslational modification,Protein methyltransferase,RNA,Cancer,Chromatin,p53
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分子量
- 452.56
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CAS-编号
- 1616392-22-3
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