A 366;A-366;5′-Methoxy-6′-[3-(1-pyrrolidinyl)propoxy]-spiro[cyclobutane-1,3′-[3H]indol]-2′-amine;5'-Methoxy-6'-[3-(1-pyrrolidinyl)propoxy]spiro[cyclobutane-1,3'-[3H]indol]-2'-amine;5'-methoxy-6'-[3-(pyrrolidin-1-yl)propoxy]spiro[cyclobutane-1,3'-indole]-2'-amine;5'-methoxy-6'-(3-(pyrrolidin-1-yl)propoxy)spiro[cyclobutane-1,3'-indol]-2'-amine;5'-Methoxy-6'-[3-(Pyrrolidin-1-Yl)propoxy]spiro[cyclobutane-1,3'-Indol]-2'-Amine;A366;GTPL8238;BKCDJTRMYWSXMC-UHFFFAOYSA-N;BCP17827;BDBM50446376;s7572;SB1;CID 76285486
Cas No.
1527503-11-2
分子式
C19H27N3O2
分子量
329.44
包装储存
Powder
-20°C
3 years
4°C
2 years
In solvent
-80°C
6 months
-20°C
1 month
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.
性状
Solid
体外研究(In Vitro)
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.
Medlife has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay
Cell Line:
MV4;11 cells
Concentration:
0.01-10 μM
Incubation Time:
14 days
Result:
Resulted in inhibited proliferation and a decrease in viability corresponding to the dose response observed for CD11b staining.
体内研究(In Vivo)
A-366 (30 mg/kg; osmotic mini-pump; daily for 14 days) treatment of MV4;11 xenografts elicits growth inhibition.
Medlife has not independently confirmed the accuracy of these methods. They are for reference only.
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.