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PluriSIn 1

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Chemical Structure| 91396-88-2 同义名 : N'-苯基异烟肼 ;PluriSln 1;NSC 14613;PluriSln #1;N’-phenyl-hydrazine-Isonicotinic acid;PluriSIn #1
CAS号 : 91396-88-2
货号 : A230785
分子式 : C12H11N3O
纯度 : 99%+
分子量 : 213.235
MDL号 : MFCD02344904
存储条件：

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(492.41 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • Dehydrogenase
描述 Human pluripotent stem cells (hPSCs) are characterized by their abilities to self-renew and to differentiate into all cell types of the human body. PluriSIn1 is an N-acyl phenylhydrazine derivative that inhibits stearoyl-coA desaturase (SCD1), a key enzyme in oleic acid biosynthesis in hPSCs. The exposure of embryonic stem cells (ESCs) with 20μM PluriSIn1 for 16 hours resulted in a gradual and significant increase of apoptotic cells. ESCs treated with PluriSIn1 (20μM) also showed higher expression of cleaved caspase-3, a hallmark executioner of apoptosis, compared to the controls. By treating hPSCs with pancaspase inhibitor Z-VAD-FMK, PluriSIn1 (20μM)-induced cell death was significantly suppressed. Also in hPSCs, 20μM PluriSIn1 led to a ∼3.5-fold elevation in the expression of the spliced isoform sXBP1 and an increase of eIF2α phosphorylation. The incubation with PluriSIn1 (20μM) for 12 hours induced ∼30% protein synthesis attenuation in hPSCs but not in differentiated cells. Moreover, the exposure of undifferentiated hPSCs with PluriSIn1 (20μM) caused a 65% reduction in SCD1 activity as compared to DMSO-treated controls. When exposed to PluriSIn1 (20μM) for 24 hours, ~40% of the mouse embryos developed into high-quality blastocysts, while the rest stopped at the morula stage or developed into blastocysts without distinguished inner cell mass cells (ICMCs). In contrast, all DMSO-treated embryos in the control group developed into blastocysts with large and distinct ICMCs. Furthermore, subcutaneous injection of PluriSIn1-treated hPSCs in immune-comprised mice failed to generate teratoma in vivo[3]. Nanog is a marker for both cell pluripotency and tumor progression. PluriSin1 treatment at 20 µM for 1 day significantly induces the apoptosis of Nanog-positive induced pluripotent stem cells derivates (iPSD). In addition, PluriSin1 treatment at 20 µM for 4 days diminished Nanog-positive stem cells in cultured iPSD while not increasing apoptosis of iPS-derived cardiomyocytes (CM)[4].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

4.69mL

0.94mL

0.47mL

23.45mL

4.69mL

2.34mL

46.90mL

9.38mL

4.69mL
参考文献

[1]Zhang L, Pan Y, et al. Inhibition of stearoyl-coA desaturase selectively eliminates tumorigenic Nanog-positive cells: improving the safety of iPS cell transplantation to myocardium. Cell Cycle. 2014;13(5):762-71.

[2]Ben-David U, Gan QF, et al. Selective elimination of human pluripotent stem cells by an oleate synthesis inhibitor discovered in a high-throughput screen. Cell Stem Cell. 2013 Feb 7;12(2):167-79.

[3]Ben-David U, Gan QF, Golan-Lev T, Arora P, Yanuka O, Oren YS, Leikin-Frenkel A, Graf M, Garippa R, Boehringer M, Gromo G, Benvenisty N. Selective elimination of human pluripotent stem cells by an oleate synthesis inhibitor discovered in a high-throughput screen. Cell Stem Cell. 2013 Feb 7;12(2):167-79.

[4]Zhang L, Pan Y, Qin G, Chen L, Chatterjee TK, Weintraub NL, Tang Y. Inhibition of stearoyl-coA desaturase selectively eliminates tumorigenic Nanog-positive cells: improving the safety of iPS cell transplantation to myocardium. Cell Cycle. 2014;13(5):762-71.