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首页-小分子抑制剂&激动剂-Epigenetics-HDAC-R306465
R306465

Chemical Structure : R306465

CAS No.: 604769-01-9

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R306465 (JNJ-16241199, R-306465)

货号: PC-27078Not For Human Use, Lab Use Only.

R306465 (JNJ-16241199) is a selective, potent inhibitor of class I histone deacetylase (HDACs) with IC50 of 3.31 nM and 23 nM for HDAC1 and HDAC8.

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5 mg ￥1780 In stock
10 mg ￥2780 In stock
25 mg ￥4780 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

R306465 (JNJ-16241199) is a selective, potent inhibitor of class I histone deacetylase (HDACs) with IC50 of 3.31 nM and 23 nM for HDAC1 and HDAC8.
R306465 inhibits the class I HDAC8 at least 10 times more potently than vorinostat and panobinostat.
R306465 preferentially inhibits deacetylation of HDAC1/HDAC3 substrate B61 in rat liver HDAC preparation with IC50 of 51 nM, much weaker acitvity against HDAC6-specific substrate B12.
R306465 is a specific inhibitor of HDAC1/3 in A2780 tumour cells, induced H3 acetylation and p21waf1, cip1 induction at concentrations as low as 100 nM in human A2780 ovarian carcinoma cells, but not HDAC6 activity.
R306465 has broad-spectrum antiproliferative activity against solid and haematological cancer cell lines (A2780 proliferation IC50=39 nM).
R306465 induces apoptosis and inhibits angiogenesis in A2780 ovarian carcinoma cells, inhibits the growth of HUVECs with an IC50 of 186 nM.
R306465 (40 mpk, p.o. once daily, vehicle: 20% HP-β-CD) induces histone acetylation and activates the p21waf1,cip1 promoter in nude mice were injected s.c. with A2780 ovarian carcinoma cells.
R306465 (20/40 mpk, p.o. vehicle: 20% HP-β-CD) inhibits tumour growth in the A2780 ovarian xenograft model, and lung (H460) and colon (HCT116) xenograft models.

物理化学性质&存储条件

分子量 413.45
分子式 C19H19N5O4S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

N-Hydroxy-2-(4-(naphthalen-2-ylsulfonyl)piperazin-1-yl)pyrimidine-5-carboxamide

参考文献

1. Arts J, et al. Br J Cancer. 2007 Nov 19;97(10):1344-53.

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