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Cat. No.: HY-116605

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GSK926

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.

CAS No.: 1346704-13-9
Formula: C₂₉H₃₅N₇O₂
Molecular Weight:513.63

Storage:

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

Data Sheet (270 KB)

GSK926 Chemical Structure

CAS No.: 1346704-13-9

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
Chemical Information
Protocols (1)
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
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Biological Activity

Description

IC₅₀ & Target

^[1]

EZH2

0.02 μM (IC₅₀)

All Histone Methyltransferase Isoforms :

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]

Chemical Information

CAS No. 1346704-13-9
Molecular Weight 513.63
Formula C₂₉H₃₅N₇O₂
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.

Protocols

All Cell Biology

Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (270 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
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]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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MOQ

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100 mg

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