您好,欢迎来到化工原料网! [登录] [免费注册]
化工原料网
位置:首页 > 产品库 > BIX-01294 trihydrochloride
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
BIX-01294 trihydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
BIX-01294 trihydrochloride图片
CAS NO:1392399-03-9
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
BIX-01294 trihydrochloride 是一种可逆且高度选择性的G9aGLP组蛋白甲基转移酶抑制剂,IC50分别为 1.9 μM 和 0.7 μM。BIX-01294 trihydrochloride 通过与底物赖氨酸残基 N 端的氨基酸竞争结合来抑制 G9a/GLP。BIX-01294 trihydrochloride 是一种 (1H-1,4-diazepin-1-yl)-quinazolin-4-yl 胺衍生物,可诱导坏死性凋亡 (necroptosis) 和自噬。BIX-01294 trihydrochloride 在复发性肿瘤细胞中具有抗肿瘤活性。
生物活性

BIX-01294 trihydrochloride is a reversible and highly selectiveG9a and GLPHistone Methyltransferaseinhibitor, withIC50s of of 1.7 μM and 0.9 μM, respectively. BIX-01294 trihydrochloride inhibits G9a/GLP by competing for binding with theamino acidsN-terminal of the substrate lysine residue. BIX-01294 trihydrochloride, a (1H-1,4-diazepin-1-yl)-quinazolin-4-yl amine derivative, inducesnecroptosisandautophagy. BIX-01294 trihydrochloride has antitumor activity in recurrent tumor cells[1][2][3][4][5].

IC50& Target

IC50: 2.7 μM (G9a in DELFIA assay)[2]
IC50: 1.9 μM for G9a and 0.7 μM for GLP[5]

体外研究
(In Vitro)

BIX-01294 (2 μM; 48 h) trihydrochloride selectively inhibits recurrent tumor cell growth[1].
BIX-01294 (1 μM) trihydrochloride leads to a marked increase in phosphorylation of S345 of MLKL[1].
BIX-01294 (1 μM) trihydrochloride significantly upregulates the canonical p53 targets Cdkn1a (p21) and Gadd45a in recurrent tumor cell lines[1].
BIX-01294 (1 μM; 6 days) trihydrochloride causes the reduction in H3K9me2 levels in primary and recurrent tumor cells[1].
BIX-01294 trihydrochloride leads to necroptotic cell death in recurrent tumor cells. Necrostatin-1 (30 μM) partially reverses cell death induced by BIX-01294 (750 nM; 24 h) trihydrochloride[1].
BIX-01294 (4.1 μM; for 2 days) trihydrochloride causes around a 20% reduction, concomitant with a comparable increase in the unmodified H3K9 fragment in H3K9me2 in mouse ES cells. BIX-01294 trihydrochloride causes pronounced reduction in H3K9me2 and a small decrease for H3K9me3 and H3K9me1 in wild-type ES cells[2].
BIX-01294 trihydrochloride has no inhibition of the other histone methyltransferases even at concentrations of 45 μM. BIX-01294 trihydrochloride does not affect SUV39H1 (H320R) and PRMT1 within the tested concentration range (up to 10 μM)[2].
BIX-01294 trihydrochloride inhibits G9a in an uncompetitive manner with S-adenosyl-methionine (SAM)[2].
BIX-01294 (1 μg/mL) causes reduction in the BrdU incorporation of fetal PASMCs. BIX-01294 treatment decreases the PASMCs migration induced by PDGF[3].

Cell Viability Assay[1]

Cell Line:Primary or recurrent tumor cells
Concentration:2 μM
Incubation Time:48 h
Result:Selectively inhibited recurrent tumor cell growth.
体内研究
(In Vivo)

BIX-01294 trihydrochloride (10 mg/kg; IP; three times a week for 2 weeks) significantly reduces tumor growth and tumor burden in recurrent tumor cells. Primary tumor growth is not inhibited[1].

Animal Model:Female MMTV-rtTA;TetO-Her2/neu (MTB;TAN) and TetO-Her2/neu (TAN) mice with recurrent or primary tumor cells[1]
Dosage:10 mg/kg
Administration:IP; three times a week for 2 weeks
Result:Significantly reduced tumor growth and tumor burden in recurrent tumor cells.
Primary tumor growth was not inhibited.
Slowed the growth of orthotopic recurrent tumors in athymic nude recipients.
分子量

600.02

Formula

C28H41Cl3N6O2

CAS 号

1392399-03-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.