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GNE-064

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Purity:99.81%

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COA HNMR HPLC

GNE-064

Catalog No. T60079Cas No. 1997321-20-6

GNE-064 is a selective, orally active and highly soluble inhibitor of SMARCA4, SMARCA2 and PBRM1 bromodomains 5. GNE-064 inhibits SMARCA4 with an IC50 of 0.035 μM and inhibits SMARCA2 with an EC50 of 0.10 μM. GNE-064 possess Kds with 0.01, 0.016, 0.018 and 0.049 μM for SMARCA4, SMARCA2, PBRM1 bromodomains 5 and PBRM1 bromodomains 2, repectively. GNE-064 can be used as a chemical probe for the research of drug synthesis.

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Pack Size	Price	Availability
1 mg	$58	In Stock
2 mg	$87	In Stock
5 mg	$148	In Stock
10 mg	$238	In Stock
25 mg	$397	In Stock
50 mg	$567	In Stock
100 mg	$768	In Stock
500 mg	Inquiry	In Stock
1 mL x 10 mM (in DMSO)	$155	In Stock

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Product Introduction

Bioactivity

Description	GNE-064 is a selective, orally active and highly soluble inhibitor of SMARCA4, SMARCA2 and PBRM1 bromodomains 5. GNE-064 inhibits SMARCA4 with an IC50 of 0.035 μM and inhibits SMARCA2 with an EC50 of 0.10 μM. GNE-064 possess Kds with 0.01, 0.016, 0.018 and 0.049 μM for SMARCA4, SMARCA2, PBRM1 bromodomains 5 and PBRM1 bromodomains 2, repectively. GNE-064 can be used as a chemical probe for the research of drug synthesis.
In vitro	GNE-064 (0-0.5 μM; 1 h) inhibits SMARCA2 in ZsGreen-SMARCA2 BD-expressing U2OS cells[1].
In vivo	GNE-064 (0.5 and 1.0 mg/kg; i.v. and p.o. once ) exibits ideal pharmacokinetics value in female CD-1 mice [1].
Alias	GNE064

Chemical Properties

Molecular Weight	327.38
Formula	C17H21N5O2
Cas No.	1997321-20-6

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 112.5mg/mL (343.6mM)

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	3.0546 mL	15.2728 mL	30.5455 mL	152.7277 mL
5 mM	0.6109 mL	3.0546 mL	6.1091 mL	30.5455 mL
10 mM	0.3055 mL	1.5273 mL	3.0546 mL	15.2728 mL
20 mM	0.1527 mL	0.7636 mL	1.5273 mL	7.6364 mL
50 mM	0.0611 mL	0.3055 mL	0.6109 mL	3.0546 mL
100 mM	0.0305 mL	0.1527 mL	0.3055 mL	1.5273 mL

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Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

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Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

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mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O TargetMol | reagent

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