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ISA-2011B

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Chemical Structure| 1395347-24-6 同义名 : -
CAS号 : 1395347-24-6
货号 : A899194
分子式 : C22H18ClN3O4
纯度 : 98+%
分子量 : 423.849
MDL号 : MFCD30533398
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(247.73 mM),配合低频超声助溶,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
描述 Phosphatidylinositol 4,5-biphosphate kinases (PIP5Ks) are a family of lipid kinases that phosphorylate phosphatidylinositol 4-phosphate on the D5 position of the inositol ring, thus inducing the production of phosphatidylinositol 4,5-biphosphate (PIP2). PIP5K1α is a lipid kinase that acts on PI3K/AKT/PTEN pathways, and thereby regulates cell survival and migration. ISA-2011B is a PIP5Kα inhibitor with promising anticancer effects. Tumor xenografts established with human prostatic carcinoma cell line 22Rv1 were treated with ISA-2011B(40 mg/kg, 2 weeks) and showed a 3.5-fold smaller tumor volumes compared with those treated with vehicle control (mean volume of tumors were 844.12 mm3 and 243.77 mm3 for vehicle-treated and ISA-2011B-treated groups, respectively)[3]. ISA-2011B treatment at 20 mM or 50 mM diminished AR-V7, CDK1 and PSA expression in PIP5K1α-overexpressing and control 22Rv1 cells, and inhibited AR-V7 and pAKT expression in PC3 cells, respectively[3]. ISA-2011B treatment at 10 µM for 6h or 24h significantly impaired the increases in mRNA levels of IL-6, IL-8, and IL-17A in T lymphocytes from healthy donors which were induced by CD38 stimulation[4]. ISA-2011B at 20 μM dramatically inhibited pSer-473 AKT by 75.55% compared with control in LNCaP cells[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.36mL

0.47mL

0.24mL

11.80mL

2.36mL

1.18mL

23.59mL

4.72mL

2.36mL

参考文献

[1]Kunkl M, Porciello N, et al. ISA-2011B, a Phosphatidylinositol 4-Phosphate 5-Kinase α Inhibitor, Impairs CD28-Dependent Costimulatory and Pro-inflammatory Signals in Human T Lymphocytes. Front Immunol. 2017 Apr 26;8:502.

[2]Sarwar M, Semenas J, et al. Targeted suppression of AR-V7 using PIP5K1α inhibitor overcomes enzalutamide resistance in prostate cancer cells. Oncotarget. 2016 Sep 27;7(39):63065-63081.

[3]Sarwar M, Semenas J, Miftakhova R, Simoulis A, Robinson B, Gjörloff Wingren A, Mongan NP, Heery DM, Johnsson H, Abrahamsson PA, Dizeyi N, Luo J, Persson JL. Targeted suppression of AR-V7 using PIP5K1α inhibitor overcomes enzalutamide resistance in prostate cancer cells. Oncotarget. 2016 Sep 27;7(39):63065-63081. doi: 10.18632/oncotarget.11757. PMID: 27588408; PMCID: PMC5325347.

[4]Kunkl M, Porciello N, Mastrogiovanni M, Capuano C, Lucantoni F, Moretti C, Persson JL, Galandrini R, Buzzetti R, Tuosto L. ISA-2011B, a Phosphatidylinositol 4-Phosphate 5-Kinase α Inhibitor, Impairs CD28-Dependent Costimulatory and Pro-inflammatory Signals in Human T Lymphocytes. Front Immunol. 2017 Apr 26;8:502. doi: 10.3389/fimmu.2017.00502. PMID: 28491063; PMCID: PMC5405084.

[5]Semenas J, Hedblom A, Miftakhova RR, Sarwar M, Larsson R, Shcherbina L, Johansson ME, Härkönen P, Sterner O, Persson JL. The role of PI3K/AKT-related PIP5K1α and the discovery of its selective inhibitor for treatment of advanced prostate cancer. Proc Natl Acad Sci U S A. 2014 Sep 2;111(35):E3689-98. doi: 10.1073/pnas.1405801111. Epub 2014 Jul 28. PMID: 25071204; PMCID: PMC4156761.