GSK926

Cat. No.: HY-116605: FAQs
Data Sheet Handling Instructions

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GSK926 (compound 3) is a selective histone lysine methyltransferase EZH2 inhibitor (IC₅₀=0.02 μM; K_i=7.9 nM), with SAM-competitive and cell-active properties. GSK926 can be used in cancer research.

For research use only. We do not sell to patients.

GSK926 Chemical Structure

CAS No. : 1346704-13-9

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•Related Small Molecules:

•Related Proteins:

View All Histone Methyltransferase Isoform Specific Products:

View All Isoforms

EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

EZH2

0.02 μM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
HCC1806	IC₅₀	324 nM Compound: 3, GSK926	Inhibition of EZH2-mediated nuclear H3K27 methylation in human HCC1806 cells after 72 hrs by immunofluorescence analysis Inhibition of EZH2-mediated nuclear H3K27 methylation in human HCC1806 cells after 72 hrs by immunofluorescence analysis	[PMID: 24900432]
LNCaP	IC₅₀	4.5 μM Compound: 3, GSK926	Inhibition of EZH2-mediated proliferation of human LNCaP cells after 6 days by chemiluminescence analysis Inhibition of EZH2-mediated proliferation of human LNCaP cells after 6 days by chemiluminescence analysis	[PMID: 24900432]

Molecular Weight

513.63

Formula

C₂₉H₃₅N₇O₂

CAS No.

1346704-13-9

SMILES

O=C(C1=CC(C2=CC=C(N3CCN(CC3)C)N=C2)=CC4=C1C=NN4C(C)C)NCC5=C(C)C=C(C)NC5=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Verma S K, et al. Identification of potent, selective, cell-active inhibitors of the histone lysine methyltransferase EZH2[J]. ACS medicinal chemistry letters, 2012, 3(12): 1091-1096. [Content Brief]

GSK926 Related Classifications

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The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass		Concentration		Volume		Molecular Weight *
	=		×		×

The dilution calculator equation

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)	×	Volume _(start)	=	Concentration _(final)	×	Volume _(final)
	×		=		×
C1		V1		C2		V2

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GSK9261346704-13-9GSK 926GSK-926Histone MethyltransferaseSelectiveInhibitorsMethyltransferasesSAMCancerInhibitorinhibitorinhibit

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