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313984-77-9

中文名稱 PU-02; PU02
英文名稱 6-[(1-NaphthalenylMethyl)thio]-9H-purine
CAS 313984-77-9
分子式 C16H12N4S
分子量 292.36
MOL 文件 313984-77-9.mol
更新日期 2024/12/15 19:35:15
313984-77-9 結(jié)構(gòu)式 313984-77-9 結(jié)構(gòu)式

基本信息

中文別名
化合物PU-02
6-((萘-1-基甲基)硫基)-7H-嘌呤
英文別名
PU 02
PU-02
PU02
6-[(1-NaphthalenylMethyl)thio]-9H-purine
6-((Naphthalen-1-ylmethyl)thio)-7H-purine
9H-Purine, 6-[(1-naphthalenylmethyl)thio]-
6-(Naphthalen-1-ylmethylsulfanyl)-7H-purine

物理化學(xué)性質(zhì)

儲(chǔ)存條件Sealed in dry,2-8°C
溶解度Soluble to 100 mM in DMSO
形態(tài)粉末
顏色White to off-white

常見問題列表

生物活性
PU02 是 6-MP (HY-13677) 的一個(gè)衍生物，是 5-HT3 受體的負(fù)變構(gòu)調(diào)節(jié)劑，其在 HEK293 細(xì)胞測(cè)得的轉(zhuǎn)染 5-HT3A 和 5-HT3AB 受體后的 IC50 值分別為 0.36 和 0.73 μM。
靶點(diǎn)

5-HT 3A Receptor

0.36 μM (IC 50 )

5-HT 3 AB

0.73 μM (IC 50 )

體外研究

PU02 (NMMP) (0-200 μM) leads to a steady decrease in cell viability of HepG2 cells (IC 50 =48.585 μM). PU02 (NMMP) shows less toxicity on L02 cells than did 6-MP after 48 h of treatment.
PU02 (NMMP) at 6.25 or 25 μM exhibits inhibitory effects on the viability of the tested cell lines, including SMMC-7721, MDA-MB-231, RKO and HCT-8 cells.
PU02 (NMMP) induces cell cycle arrest at the G2/M phase. PU02 (NMMP) downregulats the expression of cyclin B1/D1 and CDK4 in a time-dependent manner in HepG2 cells,but the expression of cyclin E is not affected.
PU02 (NMMP)-treated cells exhibits a significant increase in caspase-3 cleavage, suggesting enhanced apoptotic activity.

Apoptosis Analysis

Cell Line: HepG2 cells.
Concentration: 6.26, 12.5, 25, 50 μM.
Incubation Time: 6, 12, 24, 36 h.
Result: Induced mitochondria-dependent apoptosis.
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