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188532-26-5

中文名稱 NL-1
英文名稱 NL 1
CAS 188532-26-5
分子式 C18H25NO3S
分子量 335.46
MOL 文件 188532-26-5.mol
更新日期 2024/12/15 19:35:20
188532-26-5 結構式 188532-26-5 結構式

基本信息

中文別名
化合物NL-1
5-(3,5-二叔丁基-4-羥基芐基)噻唑烷-2,4-二酮
英文別名
NL 1
2,4-Thiazolidinedione, 5-[[3,5-bis(1,1-dimethylethyl)-4-hydroxyphenyl]methyl]-

物理化學性質

沸點446.5±40.0 °C(Predicted)
密度1.167±0.06 g/cm3(Predicted)
儲存條件Sealed in dry,Store in freezer, under -20°C
溶解度DMSO: 250 mg/mL (745.25 mM)
酸度系數(shù)(pKa)6.34±0.50(Predicted)
形態(tài)Solid
顏色White to off-white

安全數(shù)據(jù)

危險性符號(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險性描述H302-H312-H332

常見問題列表

生物活性
NL-1 是一種具有抗白血病作用的 mitoNEET 抑制劑。NL-1 抑制 REH 和 REH/Ara-C 細胞生長，IC50 分別為 47.35 μM 和 56.26 μM。NL-1 介導的白血病細胞死亡需要激活自噬途徑。
靶點

MitoNEET

體外研究

NL-1 (10-100 μM; 72 hours; REH, REH/Ara-C and ALL cell lines) treatment reduces the number of viable cells in REH, REH/Ara-C and ALL (SUP-B15, TOM-1, JM1, NALM-1, NALM-6, BV-173) cell lines, in a concentration-dependent manner. NL-1 inhibits SUPB15, NALM6 with IC 50 s of 29.48 μM, 94.26 μM, respectively. TOM1, BV173, NALM1 and JM1 all have similar IC 50 values of around 60 μM for NL-1.
NL-1 (60 μM; 6 hours; REH, REH/Ara-C cell lines) treatment mediates autophagy, and inhibition of autophagy partially decreased NL-1-induced tumor cell death.
NL-1 pretreatment inhibits the chemotactic ability of both REH and REH/Ara-C cells to migrate towards multiple chemoattractants. The cells treated with NL1 shows a dose-dependent decrease in chemotaxis both in the REH and the REH/AraC cells.

Cell Proliferation Assay

Cell Line: REH, REH/Ara-C and ALL (SUP-B15, TOM-1, JM1, NALM-1, NALM-6, BV-173) cell lines
Concentration: 10 μM, 20 μM, 30 μM, 40 μM, 50 μM, 60 μM, 70 μM, 80 μM, 100 μM
Incubation Time: 72 hours
Result: Reduced the number of viable cells in REH, REH/Ara-C and ALL (SUP-B15, TOM-1, JM1, NALM-1, NALM-6, BV-173) cell lines, in a concentration-dependent manner.

Cell Autophagy Assay

Cell Line: REH, REH/Ara-C cell lines
Concentration: 60 μM
Incubation Time: 6 hours
Result: Induced cell autophagy.
體內研究

NL-1 (10 mg/kg; intraperitoneal injection; daily; for 5 days; female NSG mice) treatment shows antileukemic activity in an in vivo mouse ALL model.

Animal Model: 10 female NOD.Cg- Prkdc scid Il2rg tm1Wjl /SzJ (NSG) mice (6-8 month old) injected with TOM-1 ALL cells
Dosage: 10 mg/kg
Administration: Intraperitoneal injection; daily; for 5 days
Result: Showed antileukemic activity in an in vivo mouse ALL model.
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