BIX 01294

製品コードS8006 バッチS800602

化学情報

	Synonyms	N/A	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₂₈H₃₈N₆O₂.3HCl
	分子量	600.02	CAS No.	1392399-03-9
Solubility (25°C)*	体外	DMSO	100 mg/mL (166.66 mM)
		Water	100 mg/mL (166.66 mM)
		Ethanol	100 mg/mL (166.66 mM)
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck 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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	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. BIX01294 induces autophagy. BIX01294 also inhibits H3K36 methylation by oncoproteins NSD1, NSD2 and NSD3.
in vitro	BIX01294 is a selective inhibitor of G9a histone methyltransferase and does not affect SUV39H1(H320R) and PRMT1 within the tested concentration range. BIX-01294 specifically inhibited G9a (H3K9me2) and, to a lesser extent, the closely related GLP enzyme (primarily H3K9me3), with an IC50 of 1.7 μM for G9a and 38 μM for GLP. BIX-01294 inhibits G9a in an uncompetitive manner with SAM. BIX-01294 (4.1μM) reduces H3K9me2 Levels in Bulk Histone Preparations from wt ES cells, mouse embryonic fibroblasts and HeLa cells, but not in G9a deficient stem cells. BIX-01294 is a valuable inhibitor for the transient modulation of chromosomal H3K9me2. BIX-01294 Reduces H3K9me2 at Several G9a Target Genes including Bim1 and Serac1. ^[1] BIX01294 could reactivate expression of HIV-1 from latently infected cells such as ACH-2 and OM10.1. ^[2]

製品説明

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. BIX01294 induces autophagy. BIX01294 also inhibits H3K36 methylation by oncoproteins NSD1, NSD2 and NSD3.

in vitro

BIX01294 is a selective inhibitor of G9a histone methyltransferase and does not affect SUV39H1(H320R) and PRMT1 within the tested concentration range. BIX-01294 specifically inhibited G9a (H3K9me2) and, to a lesser extent, the closely related GLP enzyme (primarily H3K9me3), with an IC50 of 1.7 μM for G9a and 38 μM for GLP. BIX-01294 inhibits G9a in an uncompetitive manner with SAM. BIX-01294 (4.1μM) reduces H3K9me2 Levels in Bulk Histone Preparations from wt ES cells, mouse embryonic fibroblasts and HeLa cells, but not in G9a deficient stem cells. BIX-01294 is a valuable inhibitor for the transient modulation of chromosomal H3K9me2. BIX-01294 Reduces H3K9me2 at Several G9a Target Genes including Bim1 and Serac1. ^[1]

BIX01294 could reactivate expression of HIV-1 from latently infected cells such as ACH-2 and OM10.1. ^[2]

プロトコル(参考用のみ)

キナーゼアッセイ	HMTase Assays
キナーゼアッセイ	Dissociation Enhanced Lanthanide Fluoro-ImmunoAssays (DELFIA) are performed in white, opaque 384-well plates coated with Neutravidin. Test compounds are diluted to 12 μg/ml in 50mM Tris-HCl pH 8.5containing 4% DMSO and 10 μl isdispensed into the wells. Blank and control wells received only compound buffer. GST-G9a at 10 μg/ml and SAM at 40 μM are diluted in 50mM Tris HCl pH 8.5/10 mM DTT and added in a volume of 20 μL. Blank wells received Tris/DTT buffer only. The reactions are initiated by the addition of 800 nM H3(1-20)-cysbiotin substrate in 50 mM Tris pH 8.5 in a volume of 10 μl, and incubated at room temperature for 60 minutes. The plates are washed 3 times with 100 μl of Wash Buffer. Next, 50 μl of Fluoroimmunoassay (FI) Buffer containing 5ng α-2X-di-meth H3-K9 and 5ng goat anti-rabbit Eu chelate isadded to all wells of the plate, and the plate isincubated for an additional hour at room temperature. The plates are washed 3 times with 100 μL of Wash Buffer, and 50 μl of Enhancement Solution isadded to each well. Time resolved fluorescence ismeasured after 45 minutes on a Viewlux Microplate Imager imaging for 15 second.
細胞アッセイ	細胞株	Various tumor cells
	濃度
	反応時間	48 h
	実験の流れ	Cells were allowed to grow overnight prior to 48 h treatment with increasing concentrations of BIX-01294.
動物実験	動物モデル	TetO-Her2/neu (TAN) mice
	投薬量	10 mg/kg
	投与方法	i.p.

参考

カスタマーフィードバック

: Data from [Data independently produced by , , J Pineal Res, 2018, 65(2):e12497]

: Data from [Data independently produced by , , Cancer Res, 2015, 75(11):2375-86. ]

: Data from [Data independently produced by , , PLoS One, 2015, 10(9):e0138390]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Extensive embryonic patterning without cellular differentiation primes the plant epidermis for efficient post-embryonic stomatal activities [ Dev Cell, 2023, 58(6):506-521.e5]	PubMed: 36931268
Depletion of G9A attenuates imiquimod-induced psoriatic dermatitis via targeting EDAR-NF-κB signaling in keratinocyte [ Cell Death Dis, 2023, 14(9):627]	PubMed: 37739945
Depletion of G9A attenuates imiquimod-induced psoriatic dermatitis via targeting EDAR-NF-κB signaling in keratinocyte [ Cell Death Dis, 2023, 14(9):627]	PubMed: 37739945
Perturbations in 3D genome organization can promote acquired drug resistance [ Cell Rep, 2023, 42(10):113124]	PubMed: 37733591
Restricting epigenetic activity promotes the reprogramming of transformed cells to pluripotency in a line-specific manner [ Cell Death Discov, 2023, 9(1):245]	PubMed: 37452056
Telomeres cooperate in zygotic genome activation by affecting DUX4/Dux transcription [ iScience, 2023, 26(3):106158]	PubMed: 36843839
The CHCHD2/Sirt1 corepressors involve in G9a-mediated regulation of RNase H1 expression to control R-loop [ Cell Insight, 2023, 2(4):100112]	PubMed: 37388553
Direct chemical reprogramming of human cord blood erythroblasts to induced megakaryocytes that produce platelets [ Cell Stem Cell, 2022, 29(8):1229-1245.e7]	PubMed: 35931032
Epigenetic alterations of CXCL5 in Cr(VI)-induced carcinogenesis [ Sci Total Environ, 2022, 838(Pt 1):155713]	PubMed: 35660107
BRD4770 functions as a novel ferroptosis inhibitor to protect against aortic dissection [ Pharmacol Res, 2022, 177:106122]	PubMed: 35149187

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。