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BIX-01294

產(chǎn)品活性：BIX-01294 是一種可逆且高度選擇性的 G9a 和 GLP 組蛋白甲基轉(zhuǎn)移酶抑制劑，IC₅₀ 分別為 1.9 μM 和 0.7 μM。BIX-01294 通過與底物賴氨酸殘基 N 端的氨基酸競(jìng)爭(zhēng)結(jié)合來(lái)抑制 G9a/GLP。BIX-01294 是一種 (1H-1,4-diazepin-1-yl)-quinazolin-4-yl 胺衍生物，可誘導(dǎo)壞死性凋亡 (necroptosis) 和自噬。BIX-01294 在復(fù)發(fā)性腫瘤細(xì)胞中具有抗腫瘤活性。

研究領(lǐng)域：Epigenetics  |  Autophagy

作用靶點(diǎn)：Histone Methyltransferase  |  Autophagy

In Vitro: BIX-01294 (2 μM; 48 h) selectively inhibits recurrent tumor cell growth.
BIX-01294 (1 μM) leads to a marked increase in phosphorylation of S345 of MLKL.
BIX-01294 (1 μM) significantly upregulates the canonical p53 targets Cdkn1a (p21) and Gadd45a in recurrent tumor cell lines.
BIX-01294 (1 μM; 6 days) causes the reduction in H3K9me2 levels in primary and recurrent tumor cells.
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).
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.
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).
BIX-01294 inhibits G9a in an uncompetitive manner with S-adenosyl-methionine (SAM).
BIX-01294 (1 µg/mL) causes reduction in the BrdU incorporation of fetal PASMCs. BIX-01294 treatment decreases the PASMCs migration induced by PDGF.

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.

相關(guān)產(chǎn)品：Bioactive Compound Library Plus  |  Epigenetics Compound Library  |  Histone Modification Research Compound Library  |  Anti-Cancer Compound Library  |  Autophagy Compound Library  |  Reprogramming Compound Library  |  Anti-Blood Cancer Compound Library  |  Heterocyclic Compound Library  |  Membrane Protein-targeted Compound Library  |  PRMT5-IN-17  |  EZM0414  |  WDR5-IN-5  |  PRMT5-IN-22  |  Gambogenic acid  |  SGC707  |  Dot1L-IN-7  |  MS1943  |  PRMT5-IN-21  |  NSD3-IN-3  |  DCLX069  |  MAK683  |  DS-437  |  EPZ020411  |  WDR5-IN-4 TFA  |  Amodiaquine dihydrochloride  |  Furamidine  |  SMYD3-IN-2  |  UNC0642  |  Chaetocin  |  UNC0646  |  UNC0224  |  EBI-2511  |  BVT948  |  MM-401  |  CMP-5  |  EPZ-719

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