GSK126

Catalog No. A11757

GSK126是一种有效的，高选择性的，具有S-腺苷甲硫氨酸竞争性的小分子EZH2甲基转移酶活性抑制剂，可降低总体H3K27me3水平并重新激活沉默的PRC2目标基因。

Product Citations

Lucy E. Dawson, .et al. Induction of Myogenic Differentiation Improves Chemosensitivity of Chemoresistant Cells in Soft-Tissue Sarcoma Cell Lines, Sarcoma, 2020, 2020: 8647981 PMID: 32300280
Hirosumi Tamura, .et al. Evaluation of anticancer agents using patient-derived tumor organoids characteristically similar to source tissues, Oncol Rep, 2018, Aug; 40(2): 635-646 PMID: 29917168
Dupret B, .et al. The histone lysine methyltransferase Ezh2 is required for maintenance of the intestine integrity and for caudal fin regeneration in zebrafish, Biochim Biophys Acta Gene Regul Mech, 2017, Oct;1860(10):1079-1093 PMID: 28887218
Theresa Baker, .et al. Acquisition of a single EZH2 D1 domain mutation confers acquired resistance to EZH2-targeted inhibitors, Oncotarget, 2015, Oct 20; 6(32): 32646-32655 PMID: 26360609

Technical details

Catalog Num	A11757
M. Wt	526.67
Formula	C31H38N6O2
Purity	>98%
Storage	at -20°C 3 years Powder
CAS No.	1346574-57-9
Synonyms	GSK 126, GSK-126
SMILES	CC[C@H](C)N1C=C(C2=C(C=C(C=C21)C3=CN=C(C=C3)N4CCNCC4)C(=O)NCC5=C(C=C(NC5=O)C)C)C

Biological Activity

Targets

EZH2
9.9 nM

Solubility *

In vitro (25°C)	DMSO	Warmed: 3 mg/mL (5.69 mM)
	Water	Insoluble
	Ethanol	Insoluble
In vivo	4% DMSO+corn oil	0.4 mg/mL
* <1 mg/ml means slightly soluble or insoluble. * Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Preparing Stock Solutions

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.1 mM	18.99 mL	94.94 mL	189.87 mL
0.5 mM	3.8 mL	18.99 mL	37.97 mL
1 mM	1.9 mL	9.49 mL	18.99 mL
5 mM	0.38 mL	1.9 mL	3.8 mL

*The above data is based on the productmolecular weight 526.67. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.