产品
编 号：F180586
分子式：C19H27N3O2
分子量：329.44
分子式：C19H27N3O2
分子量：329.44
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
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1mg
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5mg
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10mg
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25mg
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50mg
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100mg
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结构图
CAS No: 1527503-11-2
产品详情
生物活性：
A-366 is a potent, highly selective, peptide-competitive histone methyltransferase G9a inhibitor with IC50s of 3.3 and 38 nM for G9a and GLP (EHMT1), respectively. A-366 shows >1000-fold selectivity over 21 other methyltransferases. A-366 is also a potent, nanomolar inhibitor of the Spindlin1-H3K4me3-interaction (IC50=182.6 nM). A-366 displays high affinity at human histamine H3 receptor (Ki=17 nM) and shows subtype selectivity among subsets of the histaminergic and dopaminergic receptor families.
体内研究：
A-366 (30 mg/kg; osmotic mini-pump; daily for 14 days) treatment of MV4;11 xenografts elicits growth inhibition.Animal Model:6-8 week old SCID-beige female mice (MV4;11 xenografts)
Dosage:30 mg/kg
Administration:By osmotic mini-pump; daily for 14 days
Result:A modest 45% tumor growth inhibition resulting from A-366 treatment in this model.
体外研究：
A-366 (0.01-10 μM; 14 days) induces differentiation and affects viability in MV4;11 cells.?A-366 (0.3-3 μM; 72 hours) reduces the total levels of H3K9me2 in a time and concentration dependent manner with a cellular EC50 of ~300 nM in PC-3 prostate adenocarcinoma cells. A-366 (0.01-10 μM; 4 days; HL-60 cells) results in a dose-dependent differentiation and a corresponding decrease in proliferation. DNA content analysis of A-366-treated HL-60 cells showed an accumulation of cells in G1 consistent with cytostasis.
A-366 is a potent, highly selective, peptide-competitive histone methyltransferase G9a inhibitor with IC50s of 3.3 and 38 nM for G9a and GLP (EHMT1), respectively. A-366 shows >1000-fold selectivity over 21 other methyltransferases. A-366 is also a potent, nanomolar inhibitor of the Spindlin1-H3K4me3-interaction (IC50=182.6 nM). A-366 displays high affinity at human histamine H3 receptor (Ki=17 nM) and shows subtype selectivity among subsets of the histaminergic and dopaminergic receptor families.
体内研究：
A-366 (30 mg/kg; osmotic mini-pump; daily for 14 days) treatment of MV4;11 xenografts elicits growth inhibition.Animal Model:6-8 week old SCID-beige female mice (MV4;11 xenografts)
Dosage:30 mg/kg
Administration:By osmotic mini-pump; daily for 14 days
Result:A modest 45% tumor growth inhibition resulting from A-366 treatment in this model.
体外研究：
A-366 (0.01-10 μM; 14 days) induces differentiation and affects viability in MV4;11 cells.?A-366 (0.3-3 μM; 72 hours) reduces the total levels of H3K9me2 in a time and concentration dependent manner with a cellular EC50 of ~300 nM in PC-3 prostate adenocarcinoma cells. A-366 (0.01-10 μM; 4 days; HL-60 cells) results in a dose-dependent differentiation and a corresponding decrease in proliferation. DNA content analysis of A-366-treated HL-60 cells showed an accumulation of cells in G1 consistent with cytostasis.
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