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

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].

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].

490.64

Solid

C₂₈H₃₈N₆O₂

935693-62-2

Room temperature in continental US; may vary elsewhere.

DMSO : ≥ 110 mg/mL(224.20 mM)

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

*"≥" means soluble, but saturation unknown.

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。

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。