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BIX-01294, a diazepin-quinazolinamine derivative, is a selective inhibitor of G9a histone methyl transferase (G9a HMTase) that impairs G9a HMTase and generation of H3K9me2 in vitro. It does not compete with cofactor S-adenosyl-methionine. It enhances reprogramming efficiency of neural progenitor cells to the same levels as when four transcription factors (Oct4, Klf4, Sox2 and c-Myc) were introduced to somatic cells for generation of induced pluripotent stem cells. It may replace the requirement for ectopic OCT4 (POU5F1) and cMyc respectively in pluripotent stem cell induction (iPS). Synonyms: BIX-01294; BIX 01294; BIX01294. Grades: >98%. CAS No. 935693-62-2. Molecular formula: C28H38N6O2. Mole weight: 490.64.
BIX-01294
BIX-01294 is a reversible and highly selective G9a and GLP Histone Methyltransferase inhibitor, with IC50s of of 1.7 ?M and 0.9 ?M, respectively. BIX-01294 inhibits G9a/GLP by competing for binding with the amino acids N-terminal of the substrate lysine residue. BIX-01294, a (1H-1,4-diazepin-1-yl)-quinazolin-4-yl amine derivative, induces necroptosis and autophagy. BIX-01294 has antitumor activity in recurrent tumor cells[1][2][3][4][5]. Uses: Scientific research. Group: Signaling pathways. CAS No. 935693-62-2. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg; 250 mg; 500 mg; 1 g. Product ID: HY-10587.
BIX01294 hydrochloride hydrate
Histone methyltransferases (HMT) are histone-modifying enzymes (e.g., histone-lysine N-methyltransferases and histone-arginine N-methyltransferases) that catalyze the transfer of one, two, or three methyl groups to lysine and arginine residues of histone proteins. BIX 01294 is a diazepin-quinazolinamine derivate and G9a histone methyltransferase inhibitor with IC50 of 1.9 μM and GLP inhibitor with IC50 of 0.7 μM. It less effectively inhibits the HMTase G9a-like protein and has no effect on other known HMTases. BIX 01294 was reported to function by blocking the histone binding sites. It modulates the epigenetic status of chromatin and has been used to improve the reprogramming efficiency of iPSC generation. Synonyms: BIX 01294; BIX-01294. Grades: ≥98%. CAS No. 1808255-64-2. Molecular formula: C28H38N6O2·3HCl·xH2O. Mole weight: 600.
BIX 01294 trihydrochloride
BIX 01294 is a G9a histone methyltransferase inhibitor. It enhances the induction of pluripotent stem cells from somatic cells in vitro. BIX-01294 trihydrochloride induces necroptosis and autophagy. Synonyms: BIX 01294 trihydrochloride; BIX-01294; N-(1-benzylpiperidin-4-yl)-6,7-dimethoxy-2-(4-methyl-1,4-diazepan-1-yl)quinazolin-4-amine trihydrochloride. Grades: >98%. CAS No. 1392399-03-9. Molecular formula: C28H41Cl3N6O2. Mole weight: 600.02.
HMTase Inhibitor IV, UNC0638 (2-Cyclohexyl-N-(1-isopropylpiperidin-4-yl)-6-methoxy-7-(3-(pyrrolidin-1-yl)propoxy)quinazolin-4-amine)
A cell-permeable quinazolinamine compound that acts as a potent and reversible inhibitor of G9a and GLP HMTases (histone methyltransferases) (IC50=<15 and 19nM for G9a and GLP, respectively) and displays ~15-fold greater selectivity over DNMT1 and minimally blocks the activities of JMJD2E (IC50=4.66uM) and SETD7, SETD8, PRMT3 and SUV39H2 (IC50>10uM). Shown to lower H3K9Me2 levels in MDA-MB231 cells (IC50=81nM; EC50=11.2uM for cell toxicity) and 6-fold more potent than the HMTase Inhibitor, BIX-01294. Also, affects the activities of adrenergic a1A, adrenergic a and muscarinicM2 by 90%, 69% and 64% and a panel of 26-receptors and ion-channels by <30% at 1uM. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 2mg. US Biological Life Sciences.
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iPSC Induction Enhancer II, OAC1 N-(1H-Pyrrolo[2,3-c]pyridin-5-yl)benzamide, Induced Pluripotent Stem Cells Induction Enhancer II, Oct4-Activating Compound 1)
A cell-permeable pyrrolopyridinyl-benzamide compound that is reported to enhance the efficiency of 4F/4TF-induced iPSC generation from MEFs cultured in either feeder cell-containing ESC media or in feeder-/serum-free iSF1 media (1uM OAC1 treatment starts 48h after viral transduction). OCA1 is shown to increase cellular Oct4, Nanog, Sox2, and Tet1 mRNA levels via a yet unidentified mechanism, although OAC1 is reported not affect Oct4 promoter methylation, cellular Wnt signaling, or p53 and p21 mRNA levels. Six other iPSC reprogramming improving reagents, AM580, AzaC, BIX-01294, Tranylcypromine, VPA, and Vitamin C, in comparison, do not exhibit Oct4 and Nanog promoters enhancing activity, while BIO is demonstrated to be 3.8- and 6-fold less potent than OAC1, respectively, in inducing Oct4 and Nanog transcription. Group: Biochemicals. Grades: Highly Purified. CAS No. 300586-90-7. Pack Sizes: 25mg. Molecular Formula: C??H??N?O, Molecular Weight: 237.3. US Biological Life Sciences.
Worldwide
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