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My Cart> Small Molecule Compounds > Inhibitors & Antagonists & Agonists > DNA Damage & DNA Repai > VorinostatCAS：149647-78-9
Molecular Formula：C14H20N2O3
Molecular Weight：264.32
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：HPLC≥98%
Appearance：White to off-white Solid
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| CAS | 149647-78-9 |
| Name | Vorinostat |
| Molecular Formula | C14H20N2O3 |
| Molecular Weight | 264.32 |
| Solubility | Soluble in DMSO ≥30mg/mL |
| Purity | HPLC≥98% |
| Appearance | White to off-white Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| EC | EINECS 682-505-1 |
| MDL | MFCD00945317 |
| SMILES | O=C(NC1=CC=CC=C1)CCCCCCC(NO)=O |
| InChIKey | WAEXFXRVDQXREF-UHFFFAOYSA-N |
| InChI | InChI=1S/C14H20N2O3/c17-13(15-12-8-4-3-5-9-12)10-6-1-2-7-11-14(18)16-19/h3-5,8-9,19H,1-2,6-7,10-11H2,(H,15,17)(H,16,18) |
| PubChem CID | 5311 |
| Target Point | HDAC |
| Passage | DNA Damage/DNA Repair;Epigenetics;NF-κB |
| Background | Vorinostat is a potent HDAC inhibitor. Vorinostat can induce apoptosis. Vorinostat is also a potent inhibitor of human papillomavirus (HPV)-18 DNA amplification. |
| Biological Activity | Vorinostat 是一种有效的，可口服的 HDAC1，HDAC2，HDAC3 (Class I)，HDAC7 (Class II) 和 Class IV (HDAC11) 的抑制剂，对 HDAC1/3 的 ID50 值分别为 10 nM 和 20 nM。[1-6] |
| In Vitro | 伏立诺他在处理24小时后已经以低剂量(3μM)有效抑制MES-SA细胞生长。 HDAC I类(HDAC2和3)以及II类(HDAC7)优先受这种治疗的影响。伏立诺他显著增加MES-SA细胞中p21WAF1的表达和凋亡[1]。 Vorinostat抑制SK-N-SH和SK-N-Be(2)C，IC25值分别为1μM和0.5μM[2]。 |
| In Vivo | 在注射5×106 MES-SA细胞的裸鼠中，Vorinostat(50 mg/kg /天)可使肿瘤生长减少50％以上[1]。 |
| Cell Experiment | 通过使用RIPA缓冲液(25mM Tris-HCl pH 7.6，150mM NaCl，1％NP-40，1％脱氧胆酸钠，0.1％SDS)制备细胞裂解物，并通过Bio-Rad DC蛋白质测定法测定蛋白质浓度。 。通过SDS-PAGE分离蛋白质裂解物并转移至硝酸纤维素膜。使用以下抗体和稀释液：兔抗HDAC1(1μg/ mL);兔抗HDAC2(1μg/ mL);兔抗HDAC3(9μg/ mL);兔抗HDAC7(3μg/ mL);小鼠抗p21WAF1(0.5μg/ mL)。作为二抗，兔抗小鼠和猪抗兔HRP偶联抗体的终浓度为1μg/ mL。在4℃下过夜温育用于所有一抗，然后洗涤并在室温下用二抗孵育2小时。通过增强的化学发光测定使特异性蛋白质条带可视化。为了证明蛋白质样品的等量加载，所有蛋白质印迹都被探测β-微管蛋白。 |
| Animal Experiment | 用异氟醚麻醉12周龄雄性小鼠(n = 14)，并将5×106个MES-SA细胞皮下注射到动物的右侧腹中。来自对照组的小鼠接受含有300μL空HOP-β-CD(2-羟丙基-β-环糊精)囊泡的安慰剂。另一组小鼠接受溶解于HOP-β-CD中的伏立诺他，浓度为50mg/kg /天。从注射MES-SA肿瘤细胞后第4天开始腹膜内施用空囊泡和伏立诺他。每周两次估计小鼠体重和肿瘤大小(w2×l×0.52;通过卡尺测量)。将所有小鼠治疗21天，然后通过颈椎脱位处死。将每个肿瘤作为整体分离，并确定不同的肿瘤参数。 |
| Data Literature Source | [1]. Hrzenjak A et al. Histone deacetylase inhibitor vorinostat suppresses the growth of uterine sarcomas in vitro and in vivo. Mol Cancer. 2010 Mar 4;9:49. [2]. Lautz TB，et al. The effect of vorinostat on the development of resistance to Doxorubicin in neuroblastoma.PLoS One. 2012;7(7):e40816. [3]. Richon VM，et al. A class of hybrid polar inducers of transformed cell differentiation inhibits histone deacetylases. Proc Natl Acad Sci U S A. 1998 Mar 17;95(6):3003-7. [4]. Xu WS，et al. Histone deacetylase inhibitors: molecular mechanisms of action. Oncogene. 2007 Aug 13;26(37):5541-52. [5]. Pérez-Ca amás A，et al. Sphingomyelin-induced inhibition of the plasma membrane calcium ATPase causes neurodegeneration in type A Niemann-Pick disease. Mol Psychiatry. 2017 May;22(5):711-723. [6]. Wang J，et al. Snail determines the therapeutic response to mTOR kinase inhibitors by transcriptional repression of 4E-BP1. Nat Commun. 2017 Dec 20;8(1):2207. |
| Unit | Bottle |
| Specification | 10mg 10mM*1mL in DMSO 50mg |
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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