ChemicalBook >> CAS DataBase List >>S)-1-(sec-butyl)-N-((4,6-diMethyl-2-oxo-1,2-dihydropyridin-3-yl)Methyl)-3-Methyl-6-(6-(piperazin-1-yl)pyridin-3-yl)-1H-indole-4-carboxaMide

S)-1-(sec-butyl)-N-((4,6-diMethyl-2-oxo-1,2-dihydropyridin-3-yl)Methyl)-3-Methyl-6-(6-(piperazin-1-yl)pyridin-3-yl)-1H-indole-4-carboxaMide

S)-1-(sec-butyl)-N-((4,6-diMethyl-2-oxo-1,2-dihydropyridin-3-yl)Methyl)-3-Methyl-6-(6-(piperazin-1-yl)pyridin-3-yl)-1H-indole-4-carboxaMide structure

CAS No.: 1346574-57-9

Chemical Name:: S)-1-(sec-butyl)-N-((4,6-diMethyl-2-oxo-1,2-dihydropyridin-3-yl)Methyl)-3-Methyl-6-(6-(piperazin-1-yl)pyridin-3-yl)-1H-indole-4-carboxaMide

Synonyms: GSK126;CS-694;SK 126;CPDB1065;GSK-2816126;GSK2816126A;GSK126, >=98%;e-4-carboxamide;]-N-[(4,6-dimethyL;1-[(2S)-butan-2-yL

CBNumber:: CB72645671

Molecular Formula:: C31H38N6O2

Molecular Weight:: 526.67

MDL Number:

MOL File:: 1346574-57-9.mol

Last updated:2023-06-30 15:45:59

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S)-1-(sec-butyl)-N-((4,6-diMethyl-2-oxo-1,2-dihydropyridin-3-yl)Methyl)-3-Methyl-6-(6-(piperazin-1-yl)pyridin-3-yl)-1H-indole-4-carboxaMide Properties

Melting point	>216°C (dec.)
Boiling point	823.4±65.0 °C(Predicted)
Density	1.25±0.1 g/cm3(Predicted)
storage temp.	-20°C Freezer
solubility	DMSO (Slightly), Methanol (Slightly, Heated)
pka	11.93±0.10(Predicted)
form	Solid
color	Off-White
FDA UNII	W4OGW9QZ97

SAFETY

Risk and Safety Statements

Symbol(GHS)	GHS07
Signal word	Warning
Hazard statements	H302-H317
Precautionary statements	P280-P305+P351+P338
HS Code	2933998090

S)-1-(sec-butyl)-N-((4,6-diMethyl-2-oxo-1,2-dihydropyridin-3-yl)Methyl)-3-Methyl-6-(6-(piperazin-1-yl)pyridin-3-yl)-1H-indole-4-carboxaMide price More Price(31)

Manufacturer	Product number	Product description	CAS number	Packaging	Price	Updated	Buy
Cayman Chemical	15415	GSK126 ≥98%	1346574-57-9	1mg	$62	2024-03-01	Buy
Cayman Chemical	15415	GSK126 ≥98%	1346574-57-9	5mg	$120	2024-03-01	Buy
Cayman Chemical	15415	GSK126 ≥98%	1346574-57-9	10mg	$180	2024-03-01	Buy
Tocris	6790	GSK126 ≥98%(HPLC)	1346574-57-9	5	$79	2021-12-16	Buy
TRC	G797650	GSK126	1346574-57-9	10mg	$130	2021-12-16	Buy

Product number	Packaging	Price	Buy
15415	1mg	$62	Buy
15415	5mg	$120	Buy
15415	10mg	$180	Buy
6790	5	$79	Buy
G797650	10mg	$130	Buy

S)-1-(sec-butyl)-N-((4,6-diMethyl-2-oxo-1,2-dihydropyridin-3-yl)Methyl)-3-Methyl-6-(6-(piperazin-1-yl)pyridin-3-yl)-1H-indole-4-carboxaMide Chemical Properties,Uses,Production

Biological Activity

GSK126 is an effective EZH2 methyltransferase inhibitor with IC50 being 9.9nM and high selectivity on EZH2 which is over 1000 times higher than that of the other twenty human methyltransferases.

Invitro Reaserch

GSK126 induced a 50% loss of H3K27 tri-methylation (H3K27me3) in both EZH2 wild-type and mutant DLBCL cell lines at concentrations ranging from 7–252 nM independent of EZH2 mutation status. GSK126 suppresses cell proliferation of a panel of B-cell lymphoma cell lines. Six of the seven most sensitive DLBCL cell lines harboured Y641N, Y641F or A677G EZH2 mutations (growth IC50 = 28–861 nM). 72 h treatment with 500 nM GSK126 induces transcriptional activation in sensitive cell lines.

Invivo Research

GSK126 treated once-daily for 10 days decreases global H3K27me3 and increases gene expression in subcutaneous xenografts of KARPAS-422 in a dose-dependent fashion. With daily 50 mg per kg dosing, complete tumour growth inhibition is observed. When higher dosing regimens are examined with KARPAS-422 xenografts, marked tumour regression is observed. Upon cessation of dosing, tumours in the 50 mg per kg once daily group shows tumour stasis whereas complete tumour eradication is observed in the 150 mg per kg once daily and 300 mg per kg twice per week groups. Tumour growth inhibition also correlates with statistically significant increased survival of mice bearing the more aggressive KARPAS-422 tumours, where spontaneous deaths occurres in vehicle-treated animals. No significant changes in any blood cell types at doses and times where efficacy is observed in tumour xenografts.

Description

The histone H3 lysine 27 (H3K27) methyltransferase EZH2 plays an important role in regulating gene expression, and its aberrant activity is linked to the onset and progression of cancer. GSK126 is a selective, S-adenosyl-methionine-competitive small molecule inhibitor of EZH2 methyltransferase activity (K_i = 0.57 nM; IC₅₀ = 9.9 nM versus that of EZH1: K_i = 89 nM; IC₅₀ = 680 nM). It is more than 1,000-fold selective for EZH2 over other histone methyltranferases, including both SET-domain-containing and non-SET-domain-containing methyltransferases. At concentrations of 7-252 nM, it has been shown to inhibit global H3K27 trimethylation levels and to reactivate silenced PRC2 target genes. Furthermore, GSK126 can inhibit the proliferation of EZH2 mutant DLBCL cell lines (IC₅₀ = 28-61 nM) as well as the growth of EZH2 mutant DLBCL xenografts in mice receiving a daily dose of 50 mg/kg.

Uses

GSK126 is a potent and highly selective S-adenosyl-methionine-competitive small molecule inhibitor of EZH2 methyltransferase enzyme activity. The inhibition activity of GSK126 on EZH2 activity may provide a promising treatment for EZH2 mutant lymphoma.

Uses

GSK126 is a potent and highly selective S-adenosyl-methionine-competitive small molecule inhibitor of EZH2 methyltransferase enzyme activity. The inhibition activity of GSK126 on EZH2 activity may pro vide a promising treatment for EZH2 mutant lymphoma.

Definition

ChEBI: 1-[(2S)-butan-2-yl]-N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-3-methyl-6-[6-(1-piperazinyl)-3-pyridinyl]-4-indolecarboxamide is a member of piperazines and a member of pyridines.

storage

Store at -20°C

References

1. sato, t., et al., prc2 overexpression and prc2-target gene repression relating to poorer prognosis in small cell lung cancer. sci rep, 2013. 3(1911). 2. mccabe, m.t., et al., ezh2 inhibition as a therapeutic strategy for lymphoma with ezh2-activating mutations. nature, 2012. 492(7427): p. 108-12. 3. van aller, g.s., et al., long residence time inhibition of ezh2 in activated polycomb repressive complex 2. acs chem biol, 2014. 9(3): p. 622-9. 4. yeh, c.m., et al., epigenetic silencing of arntl, a circadian gene and potential tumor suppressor in ovarian cancer. int j oncol, 2014. 45(5): p. 2101-7.

S)-1-(sec-butyl)-N-((4,6-diMethyl-2-oxo-1,2-dihydropyridin-3-yl)Methyl)-3-Methyl-6-(6-(piperazin-1-yl)pyridin-3-yl)-1H-indole-4-carboxaMide synthesis

Synthesis of S)-1-(sec-butyl)-N-((4,6-diMethyl-2-oxo-1,2-dihydropyridin-3-yl)Methyl)-3-Methyl-6-(6-(piperazin-1-yl)pyridin-3-yl)-1H-indole-4-carboxaMide from 1-(5-(4,4,5,5-TETRAMETHYL-1,3,2-DIOXABOROLAN-2-YL)PYRIDIN-2-YL)PIPERAZINE and 1H-Indole-4-carboxaMide, 6-broMo-N-[(1,2-dihydro-4,6-diMethyl-2-oxo-3-pyridinyl)Methyl]-3-Methyl-1-[(1S)-1-Methylpropyl]-

S)-1-(sec-butyl)-N-((4,6-diMethyl-2-oxo-1,2-dihydropyridin-3-yl)Methyl)-3-Methyl-6-(6-(piperazin-1-yl)pyridin-3-yl)-1H-indole-4-carboxaMide Preparation Products And Raw materials

Raw materials

1H-Indole-4-carboxaMide, 6-broMo-N-[(1,2-dihydro-4,6-diMethyl-2-oxo-3-pyridinyl)Methyl]-3-Methyl-1-[(1S)-1-Methylpropyl]- 2,5-Dibromo-3-nitro-benzoic acid 1H-Indole-4-carboxaMide,6-broMo-N-[(1,2-dihydro-4,6-diMethyl-2-oxo-3-pyridinyl)Methyl]-3-Methyl-1-(1-Methylpropyl)- 1-(5-(4,4,5,5-TETRAMETHYL-1,3,2-DIOXABOROLAN-2-YL)PYRIDIN-2-YL)PIPERAZINE 2(1H)-Pyridinone, 3-(aminomethyl)-4,6-dimethyl- (9CI)

1H-Indole-4-carboxylic acid, 6-broMo-3-Methyl-1-(1-Methylpropyl)- 1H-Indole-4-carboxylic acid,6-broMo-1-(1-Methylpropyl)-,Methyl ester 2,5-Dibromobenzoic acid 2-Methyl-3-nitrobenzoic acid 5-BROMO-2-METHYL-3-NITROBENZOIC ACID

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Preparation Products

S)-1-(sec-butyl)-N-((4,6-diMethyl-2-oxo-1,2-dihydropyridin-3-yl)Methyl)-3-Methyl-6-(6-(piperazin-1-yl)pyridin-3-yl)-1H-indole-4-carboxaMide Suppliers

Global( 164)Suppliers

Supplier	Tel	Email	Country	ProdList	Advantage
ATK CHEMICAL COMPANY LIMITED	+undefined-21-51877795	ivan@atkchemical.com	China	32480	60
career henan chemical co	+86-0371-86658258	sales@coreychem.com	China	29914	58
Biochempartner	0086-13720134139	candy@biochempartner.com	CHINA	967	58
Hubei xin bonus chemical co. LTD	86-13657291602	linda@hubeijusheng.com	CHINA	22968	58
Chongqing Chemdad Co., Ltd	+86-023-61398051 +8613650506873	sales@chemdad.com	China	39916	58
Shaanxi Dideu Medichem Co. Ltd	+86-29-87569265 +86-18612256290	1056@dideu.com	China	3683	58
Zhengzhou Alfa Chemical Co.,Ltd	+8618530059196	sale04@alfachem.cn	China	12477	58
TargetMol Chemicals Inc.	+1-781-999-5354 +1-00000000000	marketing@targetmol.com	United States	19892	58
HANGZHOU CLAP TECHNOLOGY CO.,LTD	86-571-88216897,88216896 13588875226	sales@hzclap.com	CHINA	6313	58
Dideu Industries Group Limited	+86-29-89586680 +86-15129568250	1026@dideu.com	China	29322	58

Supplier	Advantage
ATK CHEMICAL COMPANY LIMITED	60
career henan chemical co	58
Biochempartner	58
Hubei xin bonus chemical co. LTD	58
Chongqing Chemdad Co., Ltd	58
Shaanxi Dideu Medichem Co. Ltd	58
Zhengzhou Alfa Chemical Co.,Ltd	58
TargetMol Chemicals Inc.	58
HANGZHOU CLAP TECHNOLOGY CO.,LTD	58
Dideu Industries Group Limited	58

View Lastest Price from S)-1-(sec-butyl)-N-((4,6-diMethyl-2-oxo-1,2-dihydropyridin-3-yl)Methyl)-3-Methyl-6-(6-(piperazin-1-yl)pyridin-3-yl)-1H-indole-4-carboxaMide manufacturers

Image	Update time	Product	Price	Min. Order	Purity	Supply Ability	Manufacturer
	2021-07-20	GSK126 1346574-57-9	US $0.00-0.00 / KG	5mg	99%HPLC	2000tons	Shaanxi Dideu Medichem Co. Ltd
	2019-07-06	S)-1-(sec-butyl)-N-((4,6-diMethyl-2-oxo-1,2-dihydropyridin-3-yl)Methyl)-3-Methyl-6-(6-(piperazin-1-yl)pyridin-3-yl)-1H-indole-4-carboxaMide 1346574-57-9	US $1.00 / kg	1kg	95%-99%	100kg	Career Henan Chemical Co

GSK126
1346574-57-9
US $0.00-0.00 / KG
99%HPLC
Shaanxi Dideu Medichem Co. Ltd

S)-1-(sec-butyl)-N-((4,6-diMethyl-2-oxo-1,2-dihydropyridin-3-yl)Methyl)-3-Methyl-6-(6-(piperazin-1-yl)pyridin-3-yl)-1H-indole-4-carboxaMide
1346574-57-9
US $1.00 / kg
95%-99%
Career Henan Chemical Co

S)-1-(sec-butyl)-N-((4,6-diMethyl-2-oxo-1,2-dihydropyridin-3-yl)Methyl)-3-Methyl-6-(6-(piperazin-1-yl)pyridin-3-yl)-1H-indole-4-carboxaMide Spectrum

S)-1-(sec-butyl)-N-((4,6-diMethyl-2-oxo-1,2-dihydropyridin-3-yl)Methyl)-3-Methyl-6-(6-(piperazin-1-yl)pyridin-3-yl)-1H-indole-4-carboxaMide(1346574-57-9)¹HNMR

1346574-57-9(S)-1-(sec-butyl)-N-((4,6-diMethyl-2-oxo-1,2-dihydropyridin-3-yl)Methyl)-3-Methyl-6-(6-(piperazin-1-yl)pyridin-3-yl)-1H-indole-4-carboxaMide)Related Search:

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GSK126 S)-1-(sec-butyl)-N-((4,6-diMethyl-2-oxo-1,2-dihydropyridin-3-yl)Methyl)-3-Methyl-6-(6-(piperazin-1-yl)pyridin-3-yl)-1H-indole-4-carboxaMide N-[(4,6-Dimethyl-2-oxo-1,2-dihydro-3-pyridinyl)methyl]-3-methyl-1-((1S)-1-methylpropyl)-6-[6-(1-piperazinyl)-3-pyridinyl]-1H-indole-4-carboxamide GSK126, >=98% 1-(S)-sec-butyl-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-3-methyl-6-(6-(piperazin-1-yl)pyridin-3-yl)-1H-indole-4-carboxamide GSK 126 N-[(4,6-Dimethyl-2-oxo-1,2-dihydro-3-pyridinyl)methyl]-3-methyl-1-((1S)-1-methylpropyl)-6-[6-(1-piperazinyl)-3-pyridinyl]-1H-indole-4-carboxamide N-[(4,6-Dimethyl-2-oxo-1,2-dihydro-3-pyridinyl)methyl]-3-methyl-1-((1S)-1-methylpropyl)-6-[6-(1-piperazinyl)-3-pyridinyl]-1H-indole-4-carboxamide GSK126 N-[(4,6-Dimethyl-2-ox GSK126;GSK-126;GSK 126 GSK-2816126 CPDB1065 1-[(2S)-butan-2-yl]-N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-3-methyl-6-(6-piperazin-1-ylpyridin-3-yl)indole-4-carboxamide CS-694 GSK126;S)-1-(SEC-BUTYL)-N-((4,6-DIMETHYL-2-OXO-1,2-DIHYDROPYRIDIN-3-YL)METHYL)-3-METHYL-6-(6-(PIPERAZIN-1-YL)PYRIDIN-3-YL)-1H-INDOLE-4-CARBOXAMIDE EZH2 INHIBITOR;GSK-126;GSK 126;GSK2816126A GSK2816126A GSK126 (GSK2816126A) (S)-1-(sec-butyl)-N-((4,6-diMethyl-2-oxo-1,2-dihydropyridin-3-yl)Methyl)-3-Methyl-6-(6-(piperazin-1-yl)pyridin-3-yl)-1H-indole-4-carboxaMide(GSK126) ]-N-[(4,6-dimethyL 1-[(2S)-butan-2-yL -2-oxo-1H-pyridin-3-yL -6-(6-piperazin-1-yL e-4-carboxamide SK 126 1H-Indole-4-carboxamide, N-[(1,2-dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl]-3-methyl-1-[(1S)-1-methylpropyl]-6-[6-(1-piperazinyl)-3-pyridinyl]- S)-1-(sec-butyl)-N-((4,6-diMethyl-2-oxo-1,2-dihydropyridin-3-yl)Methyl)-3-Methyl-6-(6-(piperazin-1-yl)pyridin-3-yl)-1H-indole-4-carboxaMide USP/EP/BP GSK126 (GSK2816126 1346574-57-9 1345674-57-9 C31H38N6O2 Inhibitors API