GSK126 | GSK2816126A | EZH2 Inhibitor | AmBeed-信号通路专用抑制剂

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产品名称	BET ↓ ↑	bromodomain ↓ ↑	BRPF ↓ ↑	CBP/beta-catenin ↓ ↑	p300/CBP ↓ ↑	其他靶点	纯度
MS436	++ BRD4 (1), Ki: <0.085 μM BRD4 (2), Ki: 0.34 μM						99%+
CPI-203	+++ BRD4, IC50: 37 nM						98+%
GSK1324726A	+++ BRD2, IC50: 31 nM BRD4, IC50: 22 nM						99%+
PFI-1	++ BRD2, IC50: 98 nM BRD4, IC50: 0.22 μM						98%
Apabetalone	+ BD2, IC50: 0.51 μM						99%
(+)-JQ1	+++ BRD4 (2), IC50: 33 nM BRD4 (1), IC50: 77 nM						98%
I-BET151	+ BRD3, IC50: 0.25 μM BRD4, IC50: 0.5 μM						98%
Molibresib	+++ BET proteins, IC50: 35 nM						99%+
I-BRD9	+++ BRD4, pIC50: 5.3 BRD9, pIC50: 7.3						99%+
BI-7273	++++ BRD7, IC50: 117 nM BRD9, IC50: 19 nM						97%
Pelabresib	+++ BRD4-BD1, IC50: 39 nM						98%
ARV-825	+++ BRD4 BD2, Kd: 28 nM BRD4 BD1, Kd: 90 nM						99%+
Birabresib							99%+
BI 2536	+++ BRD4, Kd: 37 nM					c-Myc	99%+
Bromosporine	++ BRD2, IC50: 0.29 μM BRD9, IC50: 0.122 μM	++++ CECR2, IC50: 17 nM					99%+
XMD8-92	++ BRD4 (1), Kd: 170 nM						99%+
Mivebresib	✔						99%+
BI-9564	++++ BRD9, Kd: 5.9 nM BRD7, Kd: 73 nM	++ CECR2, Kd: 77 nM					98%
AZD5153 6-Hydroxy-2-naphthoic acid	++++ FL-BRD4, IC50: 5 nM						99%+
PLX51107	++++ BRD4 BD2, Kd: 1.7 nM BRD3 BD1, Kd: 2.1 nM						99%+
FL-411	+ BRD4(1), IC50: 0.43 μM						99%+
ABBV-744	✔						99%+
dBET6	++++ BRD4, IC50: 14 nM						99%+
dBET1	++++ BRD4, IC50: 20 nM						99%+
MZ1	++++ Brd2(BD2), Kd: 62 nM Brd3(BD2), Kd: 13 nM						99%+
dBET57	+ BRD4_BD1, DC50: 500 nM						99%+
SF2523	+ BRD4, IC50: 241 nM					DNA-PK	99%+
INCB054329	++++ BRD3-BD1, IC50: 9 nM BRD4-BD1, IC50: 119 nM						99%
INCB-057643	✔						99%+
(E/Z)-ZL0420	+++ BRD4 BD2, IC50: 32 nM BRD4 BD1, IC50: 27 nM						99%+
BMS-986158	✔						99%
BRD4 Inhibitor-10	++++ BRD4-BD2, IC50: 41 nM BRD4-BD1, IC50: 5 nM						97%
A1874	✔						99%+
Y06036	++ BRD4 (1), Kd: 82 nM						99%+
Alobresib	✔					NF-κB	95%
ODM-207	✔						98%
GSK778	+++ BRD2-BD1, IC50: 75nM BRD4-BD1, IC50: 143 nM						97%
SRX3207	+ BRD42, IC50: 3070 nM BRD41, IC50: 3070 nM					Syk	98%
GSK046	+++ BRD3_BD2, IC50: 98 nM BRD4_BD2, IC50: 214 nM						98%
GSK620	✔						97%
Trotabresib	✔						99%
NHWD-870	✔						98%
CFT8634	++++ BRD9, DC50: 3 nM						98%
GSK2801		++ BAZ2A, Kd: 257 nM BAZ2B, Kd: 136 nM					99%+
KG-501		✔					99%+
UNC 669		+ L3MBTL3, IC50: 35 μM L3MBTL4, IC50: 6 μM					99%
PFI-3		+++ SMARCA2A, Kd: 72 nM SMARCA4, Kd: 55 nM					99%+
UNC1215		+++ L3MBTL3, IC50: 120 nM L3MBTL3- D274A, IC50: 3.5 μM					99%+
EED226		++ EED, Kd: 82 nM PRC2, Kd: 114 nM					99%+
BRD9539		✔					98%
UNC926		+ L3MBTL1, Kd: 3.9 μM					99%
666-15		++ CREB, IC50: 81 nM					99%+
UNC6852		+ EED, IC50: 247 nM					98%
BAZ1A-IN-1		+ BAZ1A, Kd: 0.52 μM					99%+
PFI-4			++ BRPF2, IC50: 7.9 μM BRPF1, IC50: 80 nM				99%+
OF-1			++ BRPF1B, Kd: 100 nM BRPF2, Kd: 500 nM				99%+
GSK-5959			++ BRPF3, pIC50: 7.1 BRPF2, pIC50: 5.2				99%
GSK6853			++++ BRPF1, pIC50: 8.1				99%+
NI-42			++++ BRPF3, IC50: 260 nM BRPF1, IC50: 48 nM				99%+
E-7386				+++ CBP/beta-catenin, IC50: 0.0484 μM			99%
I-CBP112					++ CBP, Kd: 151 nM p300, Kd: 167 nM		98+%
Histone Acetyltransferase Inhibitor II					+ p300, IC50: 5 μM		98%
C646					+ p300/CBP, Ki: 400 nM		99%+
Anacardic Acid					+ p300/CBP, IC50: 8.5 μM PCAF, IC50: 5 μM		99%+
SGC-CBP30					++++ EP300, IC50: 38 nM CREBBP, IC50: 21 nM		99%+
Nordihydroguaiaretic acid					✔	IGF-1R,HER2	99%+
Curcumin					+ p300, IC50: ~25 μM	Ferroptosis,NF-κB,Nrf2	98%
CPI-637					+++ EP300, IC50: 0.051 μM CBP, IC50: 0.03 μM		99%+
Foscenvivint					✔	β-catenin	99%+
A-485					++ p300 HAT, IC50: 0.06 μM		99%+
GNE-781	+ BRD4(1), IC50: 5100 nM				++++ CBP, IC50: 0.94 nM		99%
NEO2734	+++ BET, IC50: <30 nM				+++ p300/CBP, IC50: <30 nM		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

产品名称	Histone Methyltransferase ↓ ↑	纯度
BRD4770	✔	99%+
UNC1999	+++ EZH2, IC50: 2 nM EZH1, IC50: 45 nM	99%+
EPZ005687	++ EZH2, Ki: 24 nM	98+%
EPZ015666	+++ PRMT5, Ki: 5 nM	99%+
3-Deazaneplanocin A HCl	++++ S-adenosylhomocysteine hydrolase, Ki: 50 pM	99%+
Tazemetostat	+++ EZH2, IC50: 11 nM EZH2, Ki: 2.5 nM	98%
GSK126	++ EZH2, IC50: 9.9 nM	99%+
MI-3	+ Menin-MLL, IC50: 648 nM	98%
MM-102	++ MLL1, IC50: 0.4 μM	99%
EI1	++ EZH2 (Y641F), IC50: 13 nM Ezh2 (wild-type), IC50: 15 nM	96%
SGC0946	++++ DOT1L, IC50: 0.3 nM	99%+
PFI-2 HCl	++++ SETD7, Ki: 0.33 nM SETD7, IC50: 2 nM	99%+
Pinometostat	++++ DOT1L, Ki: 80 pM	99%+
EPZ004777	+++ DOT1L, IC50: 0.4 nM	99%+
Entacapone	++ COMT, IC50: 151 nM	95%
UNC0379	+ SETD8, IC50: 7.9 μM	99%+
Menin-MLL inhibitor MI-2	+ Menin-MLL, IC50: 446 nM	98%
GSK343	+++ EZH2, IC50: 4 nM EZH1, IC50: 240 nM	99%+
BIX-01294 3HCl	+ G9a, IC50: 2.7 μM	99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

靶点	Histone Methyltransferase EZH2, IC50:9.9 nM
描述	EZH2 is the enzymatic subunit of PRC2 (Polycomb repressive complex 2), a complex that can methylate lysine 27 of histone H3 (H3K27) to promote transcriptional silencing. GSK126 is a potent inhibitor of EZH2 and inhibits both wild-type and mutant EZH2 methyltransferase activity with similar potencies (Ki^app=0.5 - 3 nM, measure by enzymatic activity) and has more than 1,000-fold selectivity for EZH2 as compared with other methyltransferases and 150-fold as compared to EZH1 (Ki^app = 89 nM). GSK126 induced a 50% loss of H3K27me3 in both EZH2 wild-type and mutant DLBCL cell lines at concentrations ranging from 7 - 252 nM independent of EZH2 mutation status (treated with GSK126 for 48h). GSK126 most potently inhibited H3K27me3, followed by H3K27me2 and H3K27me1 were only weakly reduced at the highest inhibitor concentration, with no effect on total histone H3 and PRC2 components. Following 10 days of once-daily dosing of GSK126 in mice using subcutaneous xenografts of KARPAS-422 and Pfeiffer cells, on dose 15 - 150 mg/kg, global H3K27me3 decreased and EZH2 targeted genes (TXNIP and TNFRSF21) expression increased in a dose dependent fashion. With daily 50 mg/kg dosing, complete tumor growth inhibition can be observed in both KARPAS-422 and Pfeiffer cell models. Complete tumor eradication can be observed on dose of 150 mg/kg daily or 300 mg/kg twice a week^[1].
作用机制	GSK126 is the SAM-competitive inhibitor of PRC2^[1].

Cell Line NCI-H82 cells RMG1 cells OVISE cells Primary hepatocytes BT12 cells NUH40 cells Kelly cells DLBCL cell lines KB1P-G3 KB1P-B11 SUM149 GES-1 cells A549 cells H1944 cells	Concentration	Treated Time	Description	References
NCI-H82 cells	5 μM	48 h	GSK126 partially reduced MYC expression and inhibited cell proliferation	Nat Commun. 2022 Jan 10;13(1):12.
RMG1 cells	100 nM	12 days	GSK126 selectively inhibits the growth of ARID1A knockdown cells, significantly reducing cell growth compared to controls.	Nat Med. 2015 Mar;21(3):231-8.
OVISE cells	5 μM	12 days	GSK126 significantly reduces 3D growth of ARID1A mutated cells, while the effects on ARID1A wild type cells are not significant.	Nat Med. 2015 Mar;21(3):231-8.
Primary hepatocytes	5 μM	48 h	GSK126 reversed the effects of HBx on D-GalN-induced ferroptosis in hepatocytes, leading to a rebound in SLC7A11 expression and improved cell viability, MDA, GSH, and iron levels.	J Biomed Sci. 2021 Oct 6;28(1):67.
BT12 cells	6 μM	72 h	To evaluate the effect of GSK126 on cell proliferation, the results showed that GSK126 significantly inhibited the metabolic activity of BT12 cells.	Mol Cancer Ther. 2022 May 4;21(5):715-726.
NUH40 cells	6 μM	72 h	To evaluate the effect of GSK126 on cell proliferation, the results showed that GSK126 significantly inhibited the metabolic activity of NUH40 cells.	Mol Cancer Ther. 2022 May 4;21(5):715-726.
Kelly cells	5 μM	48 h	GSK126 inhibited EZH2 methyltransferase activity but had minimal effects on MYCN expression	Nat Commun. 2022 Jan 10;13(1):12.
DLBCL cell lines	4 μM	4 days	To investigate the effect of GSK126 on MHC-I expression, results showed that GSK126 treatment significantly increased HLA-B and NLRC5 transcription	Immunity. 2021 Jan 12;54(1):116-131.e10.
KB1P-G3	7.5 µM	72 h	Single agent GSK126 treatment induced 17% reduction of viability, while the combination with AZD1390 displayed 93% cytotoxicity in BRCA1-deficient cells.	Breast Cancer Res. 2022 Jun 17;24(1):41.
KB1P-B11	7.5 µM	72 h	Single agent GSK126 treatment induced 17% reduction of viability, while the combination with AZD1390 displayed 93% cytotoxicity in BRCA1-deficient cells.	Breast Cancer Res. 2022 Jun 17;24(1):41.
SUM149	7.5 µM	72 h	Single agent GSK126 treatment induced 17% reduction of viability, while the combination with AZD1390 displayed 77-79% cytotoxicity in BRCA1-mutant cells.	Breast Cancer Res. 2022 Jun 17;24(1):41.
GES-1 cells	2 µM	72 h	Inhibited H3K27me3 methylation, reduced RPL15 expression, and attenuated Wnt signaling pathway	Cell Commun Signal. 2024 Aug 15;22(1):402.
A549 cells	5 µM	11 days	By inhibiting EZH2, GSK126 moderately activated the reporter in A549 cells, indicating it promoted partial activation of EMT.	Sci Adv. 2021 Feb 24;7(9):eabd7974.
H1944 cells	5 µM	11 days	By inhibiting EZH2, GSK126 moderately activated the reporter in H1944 cells, indicating it promoted partial activation of EMT.	Sci Adv. 2021 Feb 24;7(9):eabd7974.

Species Immunocompromised mice C57BL/6 mice Athymic mice Mice Mice	Animal Model ARID1A mutated ovarian cancer model LPS/D-GalN-induced acute liver failure model Intracranial AT/RT xenograft model Kelly xenograft model BRCA1-deficient mammary tumor model	Administration	Dosage	Frequency	Description	References
Immunocompromised mice	ARID1A mutated ovarian cancer model	Intraperitoneal injection	50 mg/kg	Daily for 3 weeks	GSK126 treatment causes regression of ARID1A mutated tumors and significantly reduces the number of tumor nodules in the peritoneal cavity.	Nat Med. 2015 Mar;21(3):231-8.
C57BL/6 mice	LPS/D-GalN-induced acute liver failure model	Intraperitoneal injection	150 mg/kg	Single dose, continued until the end of the experiment	GSK126 partially reversed the effects of HBx on LPS/D-GalN-induced acute liver failure and ferroptosis, improving liver histopathology, MDA, GSH, and iron levels.	J Biomed Sci. 2021 Oct 6;28(1):67.
Athymic mice	Intracranial AT/RT xenograft model	Intraperitoneal injection	100 mg/kg	Once daily for 20 days	To evaluate the anti-tumor effect of GSK126 in intracranial AT/RT xenograft models, the results showed that GSK126 monotherapy significantly inhibited tumor growth and prolonged the survival of mice.	Mol Cancer Ther. 2022 May 4;21(5):715-726.
Mice	Kelly xenograft model	Intraperitoneal injection	25 mg/kg, 50 mg/kg, 100 mg/kg	Once daily for 2 weeks	GSK126 at 25 mg/kg significantly inhibited H3K27me3 but had minimal effects on MYCN expression and tumor growth	Nat Commun. 2022 Jan 10;13(1):12.
Mice	BRCA1-deficient mammary tumor model	Intraperitoneal injection (GSK126), oral gavage (AZD1390)	150 mg/kg	Daily for 28 consecutive days	Combined treatment with GSK126 and AZD1390 significantly increased anti-tumor activity and prolonged progression-free survival in BRCA1-deficient mammary tumor-bearing mice.	Breast Cancer Res. 2022 Jun 17;24(1):41.

CAS号	1346574-57-9
分子式	C₃₁H₃₈N₆O₂
分子量	526.67
SMILES Code	O=C(C1=CC(C2=CC=C(N3CCNCC3)N=C2)=CC4=C1C(C)=CN4[C@@H](C)CC)NCC5=C(C)C=C(C)NC5=O
MDL No.	MFCD23381067

别名	GSK2816126A; GSK2816126
运输	蓝冰
InChI Key	FKSFKBQGSFSOSM-QFIPXVFZSA-N
Pubchem ID	68210102

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human A549 cells	Cytotoxic assay	72 h	Cytotoxicity against human A549 cells assessed as growth inhibition after 72 hrs by WST-1 assay, GI50=18.7 μM.	24767850
human Daudi cells	Cytotoxic assay	72 h	Cytotoxicity against human Daudi cells assessed as growth inhibition after 72 hrs by WST-1 assay, GI50=11.2 μM.	24767850
human HeLa cells	Function assay	72 h	Inhibition of EZH2 in human HeLa cells assessed as reduction in H3K27me3 levels incubated for 72 hrs by ELISA method, IC50=0.28 μM.	26189078
human PC3 cells	Cytotoxic assay	72 h	Cytotoxicity against human PC3 cells assessed as growth inhibition after 72 hrs by WST-1 assay, GI50=9.4 μM.	24767850
human Pfeiffer cells	Cytotoxic assay	72 h	Cytotoxicity against human Pfeiffer cells expressing EZH2 A667G mutant assessed as growth inhibition after 72 hrs by WST-1 assay, GI50=0.18 μM.	24767850
human T98G cells	Cytotoxic assay	72 h	Cytotoxicity against human T98G cells assessed as growth inhibition after 72 hrs by WST-1 assay, GI50=12.6 μM.	24767850
human U2932 cells	Cytotoxic assay	72 h	Cytotoxicity against human U2932 cells assessed as growth inhibition after 72 hrs by WST-1 assay, GI50=6.7 μM.	24767850
human U87MG cells	Cytotoxic assay	72 h	Cytotoxicity against human U87MG cells assessed as growth inhibition after 72 hrs by WST-1 assay, GI50=28.5 μM.	24767850

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