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BIX-01294
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图片
CAS NO:935693-62-2
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
10mg电议
50mg电议
100mg电议
200mg电议

产品介绍
BIX-01294 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 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 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 在复发性肿瘤细胞中具有抗肿瘤活性。
生物活性

BIX-01294 is a reversible and highly selectiveG9a and GLPHistone Methyltransferaseinhibitor, withIC50s of of 1.7 μM and 0.9 μM, respectively. BIX-01294 inhibits G9a/GLP by competing for binding with theamino acidsN-terminal of the substrate lysine residue. BIX-01294, a (1H-1,4-diazepin-1-yl)-quinazolin-4-yl amine derivative, inducesnecroptosisandautophagy. BIX-01294 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) selectively inhibits recurrent tumor cell growth[1].
BIX-01294 (1 μM) leads to a marked increase in phosphorylation of S345 of MLKL[1].
BIX-01294 (1 μM) significantly upregulates the canonical p53 targets Cdkn1a (p21) and Gadd45a in recurrent tumor cell lines[1].
BIX-01294 (1 μM; 6 days) causes the reduction in H3K9me2 levels in primary and recurrent tumor cells[1].
BIX-01294 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)[1].
BIX-01294 (4.1 μM; for 2 days) causes around a 20% reduction, concomitant with a comparable increase in the unmodified H3K9 fragment in H3K9me2 in mouse ES cells. BIX-01294 causes pronounced reduction in H3K9me2 and a small decrease for H3K9me3 and H3K9me1 in wild-type ES cells[2].
BIX-01294 has no inhibition of the other histone methyltransferases even at concentrations of 45 μM. BIX-01294 does not affect SUV39H1 (H320R) and PRMT1 within the tested concentration range (up to 10 μM)[2].
BIX-01294 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 hours
Result:Selectively inhibited recurrent tumor cell growth.
体内研究
(In Vivo)

BIX-01294 (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

490.64

性状

Solid

Formula

C28H38N6O2

CAS 号

935693-62-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : ≥ 110 mg/mL(224.20 mM)

H2O : 1 mg/mL(2.04 mM;Need ultrasonic)

*"≥" means soluble, but saturation unknown.

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.0382 mL10.1908 mL20.3815 mL
5 mM0.4076 mL2.0382 mL4.0763 mL
10 mM0.2038 mL1.0191 mL2.0382 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40%PEG300   5%Tween-80   45% saline

    Solubility: ≥ 2.75 mg/mL (5.60 mM); Clear solution

    此方案可获得 ≥ 2.75 mg/mL (5.60 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 27.5 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH2O 中,得到澄清透明的生理盐水溶液
  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20%SBE-β-CDin saline)

    Solubility: ≥ 2.75 mg/mL (5.60 mM); Clear solution

    此方案可获得 ≥ 2.75 mg/mL (5.60 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 27.5 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90%corn oil

    Solubility: ≥ 2.75 mg/mL (5.60 mM); Clear solution

    此方案可获得 ≥ 2.75 mg/mL (5.60 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 27.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在本网站选购。