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GSK3326595

Name: GSK3326595
Brand: antibodies-online
SKU: ABIN7233257
Price: 92.31 USD
Availability: InStock

Inh 1616392-22-3 6-[(1-Acetylpiperidine-4-yl)amino]-N-[(2S)-3-(3,4-dihydro-1H-isoquinolin-2-yl)-2-hydroxypropyl]pyrimidine-4-carboxamide

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Catalog No. ABIN7233257

Datasheet as PDF

Application

Inhibition (Inh)

Purpose

Selective PRMT5 inhibitor

Characteristics

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.

Purity

>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)
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

Radicicol
Inh 12772-57-5

Geldanamycin- FITC
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

Nicotinamide
Inh 98-92-0 Pyridine-3-carboxylic acid amide

5-Azacytidine
Inh Cell-permeable 320-67-2 4-Amino-1-ß-D-ribofuranosyl-1,3,5-triazin-2(1H)-one

SAHA (Vorinostat)
Inh Cell-permeable 149647-78-9 Suberoylanilide-hydroxamic acid

Phenylbutyrate Na
Inh 1716-12-7 4-Phenylbutyric acid, sodium salt

CI-994
Inh 112522-64-2 4-(Acetylamino)-N-(2-aminophenyl)benzamide

Tranylcypromine hemisulfate (±)
Inh Cell-permeable 13492-01-8 Trans (±)-2-phenylcyclopropanamine, hemisulfate salt

Tenovin-1
Inh 380315-80-0 N-[(4-Acetamidophenyl)carbamothioyl]-4-tert-butylbenzamide

Restrictions

For Research Use only
Format

Powder

Storage

-20 °C
Background

EPZ015938,Proliferation,Epigenetics,Posttranslational modification,Protein methyltransferase,RNA,Cancer,Chromatin,p53

Molecular Weight

452.56

CAS-No

1616392-22-3