G9a/GLP

阻害剤の選択性比較

カタログ番号	製品カタログ	溶解度(25°C)
カタログ番号	製品カタログ	水	DMSO	アルコール
S8006	BIX 01294	98 mg/mL	98 mg/mL	8 mg/mL
S8071	UNC0638	6 mg/mL	100 mg/mL	100 mg/mL
S7230	UNC0642	<1 mg/mL	100 mg/mL	100 mg/mL
S8068	Chaetocin	<1 mg/mL	100 mg/mL	<1 mg/mL
S7572	A-366	<1 mg/mL	65 mg/mL	65 mg/mL
S7591	BRD4770	<1 mg/mL	27 mg/mL	<1 mg/mL

G9a/GLP製品

All (6) G9a/GLP阻害剤(6)

製品コード	製品説明	文献中Selleckの製品使用例	お客様のフィードバック
S8006	BIX 01294 BIX01294 is an inhibitor of G9a histone methyltransferase with IC50 of 2.7 μM in a cell-free assay, reduces H3K9me2 of bulk histones, also weakly inhibits GLP (primarily H3K9me3), no significant activity observed at other histone methyltransferases.	Cancer Cell, 2019, 35(5):752-766 Cell Rep, 2019, 28(2):512-525.e6 Biochim Biophys Acta Gene Regul Mech, 2019, 1862(2):173-183	The H3K9me2 inhibitor BIX01294 mimics the effects of BPA and DEHP on the expression of meiotic genes and Plzf in cultured testes. (A) representative double IF staining for Mvh (green) and Stra8 (red) and Scp3 (red) and (B) Plzf (red) in histological sections of control and BIX01294-treated testes. (C) RT-qPCR analysis of Stra8, Scp3, Rec8, Spo11 and plzf in testes from the control and BIX01294-treated groups. Data are represented as the mean ± SEM. ns, P > 0.05, P < 0.05; *P < 0.01.
S8071	UNC0638 UNC0638 is a potent, selective and cell-penetrant chemical probe for G9a and GLP with IC50 of <15 nM and 19 nM, respectively, shows selectivity over a wide range of epigenetic and non-epigenetic targets.	Clin Epigenetics, 2019, 11(1):165 Biochim Biophys Acta Gene Regul Mech, 2019, 1862(2):173-183
S7230	UNC0642 UNC0642 is a potent, selective inhibitor of histone methyltransferases G9a/GLP with IC50s less than 2.5 nM for G9a and GLP and shows more than 300-fold selective for G9a and GLP over a broad range of kinases, GPCRs, transporters, and ion channels.	Clin Epigenetics, 2019, 11(1):165
S8068	Chaetocin Chaetocin, a natural product from Chaetomium species, is a histone methyltransferase inhibitor with IC50 of 0.8 μM, 2.5 μM and 3 μM for dSU(VAR)3-9, mouse G9a and Neurospora crassa DIM5, respectively.	Nat Commun, 2019, 10(1):273 Cell Death Dis, 2019, 10(12):894 Arch Biochem Biophys, 2019, 10.1016/j.abb.2019.06.010
S7572	A-366 A-366 is a potent and selective G9a/GLP histone lysine methyltransferase inhibitor with IC50 of 3.3nM, exhibiting >1000-fold selectivity for G9a/GLP over 21 other methyltransferases.	Nat Med, 2019, 25(7):1073-1081
S7591	BRD4770 BRD4770 is a histone methyltransferase G9a inhibitor with IC50 of 6.3 μM, and induces cell senescence.	Hum Pathol, 2018, 72:117-126

製品コード	製品説明	文献中Selleckの製品使用例	お客様のフィードバック
S8006	BIX 01294 BIX01294 is an inhibitor of G9a histone methyltransferase with IC50 of 2.7 μM in a cell-free assay, reduces H3K9me2 of bulk histones, also weakly inhibits GLP (primarily H3K9me3), no significant activity observed at other histone methyltransferases.	Cancer Cell, 2019, 35(5):752-766 Cell Rep, 2019, 28(2):512-525.e6 Biochim Biophys Acta Gene Regul Mech, 2019, 1862(2):173-183	The H3K9me2 inhibitor BIX01294 mimics the effects of BPA and DEHP on the expression of meiotic genes and Plzf in cultured testes. (A) representative double IF staining for Mvh (green) and Stra8 (red) and Scp3 (red) and (B) Plzf (red) in histological sections of control and BIX01294-treated testes. (C) RT-qPCR analysis of Stra8, Scp3, Rec8, Spo11 and plzf in testes from the control and BIX01294-treated groups. Data are represented as the mean ± SEM. ns, P > 0.05, P < 0.05; *P < 0.01.
S8071	UNC0638 UNC0638 is a potent, selective and cell-penetrant chemical probe for G9a and GLP with IC50 of <15 nM and 19 nM, respectively, shows selectivity over a wide range of epigenetic and non-epigenetic targets.	Clin Epigenetics, 2019, 11(1):165 Biochim Biophys Acta Gene Regul Mech, 2019, 1862(2):173-183
S7230	UNC0642 UNC0642 is a potent, selective inhibitor of histone methyltransferases G9a/GLP with IC50s less than 2.5 nM for G9a and GLP and shows more than 300-fold selective for G9a and GLP over a broad range of kinases, GPCRs, transporters, and ion channels.	Clin Epigenetics, 2019, 11(1):165
S8068	Chaetocin Chaetocin, a natural product from Chaetomium species, is a histone methyltransferase inhibitor with IC50 of 0.8 μM, 2.5 μM and 3 μM for dSU(VAR)3-9, mouse G9a and Neurospora crassa DIM5, respectively.	Nat Commun, 2019, 10(1):273 Cell Death Dis, 2019, 10(12):894 Arch Biochem Biophys, 2019, 10.1016/j.abb.2019.06.010
S7572	A-366 A-366 is a potent and selective G9a/GLP histone lysine methyltransferase inhibitor with IC50 of 3.3nM, exhibiting >1000-fold selectivity for G9a/GLP over 21 other methyltransferases.	Nat Med, 2019, 25(7):1073-1081
S7591	BRD4770 BRD4770 is a histone methyltransferase G9a inhibitor with IC50 of 6.3 μM, and induces cell senescence.	Hum Pathol, 2018, 72:117-126

Tags: G9a/GLP inhibitor | G9a/GLP activator | G9a/GLP Inhibition

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