BIX-01294 trihydrochloride

製品コードS8006 バッチS800601

印刷

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

98 mg/mL (163.32 mM)

Water

98 mg/mL (163.32 mM)

Ethanol

8 mg/mL (13.33 mM)

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension

CMC-NA

≥5mg/ml

Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

* <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	BIX-01294 trihydrochloride は、G9a histone methyltransferase の阻害剤であり、セル-フリーアッセイにおける IC50 は 2.7 μM であり、バルクヒストンの H3K9me2 を減少させ、GLP（主に H3K9me3）を弱く阻害し、他のヒストンメチルトランスフェラーゼでは有意な活性は観察されません。BIX01294 は autophagy を誘導します。BIX01294 は、オンコプロテイン NSD1、NSD2、および NSD3 による H3K36 メチル化も阻害します。
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. BIX01294 could reactivate expression of HIV-1 from latently infected cells such as ACH-2 and OM10.1.

製品説明

BIX-01294 trihydrochloride は、G9a histone methyltransferase の阻害剤であり、セル-フリーアッセイにおける IC50 は 2.7 μM であり、バルクヒストンの H3K9me2 を減少させ、GLP（主に H3K9me3）を弱く阻害し、他のヒストンメチルトランスフェラーゼでは有意な活性は観察されません。BIX01294 は autophagy を誘導します。BIX01294 は、オンコプロテイン NSD1、NSD2、および NSD3 による H3K36 メチル化も阻害します。

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.

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

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

http://www.ncbi.nlm.nih.gov/pubmed/?term=17289593
http://www.ncbi.nlm.nih.gov/pubmed/?term=20335163
https://pubmed.ncbi.nlm.nih.gov/33147463/

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：

EHMT2-mediated R-loop formation promotes the malignant progression of prostate cancer via activating Aurora B [ Clin Transl Med, 2025, 15(1):e70164]	PubMed: 39763034
BIX01294 suppresses PDAC growth through inhibition of glutaminase-mediated glutathione dynamics [ Mol Metab, 2025, 94:102113]	PubMed: 39961401
EHMT2 promotes tumorigenesis in GNAQ/11-mutant uveal melanoma via ARHGAP29-mediated RhoA pathway [ Acta Pharm Sin B, 2024, 14(3):1187-1203]	PubMed: 38486999
Gamma-glutamyl transferase secreted by Helicobacter pylori promotes the development of gastric cancer by affecting the energy metabolism and histone methylation status of gastric epithelial cells [ Cell Commun Signal, 2024, 22(1):402]	PubMed: 39148040
Oxidative stress contributes to hypermethylation of Histone H3 lysine 9 in placental trophoblasts from preeclamptic pregnancies [ Front Endocrinol (Lausanne), 2024, 15:1371220]	PubMed: 38737551
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
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

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。

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