Ricolinostat
作者：齐岳
发布时间：2023-09-05
08:53:47
点击数：
产品名称：Ricolinostat
产品描述：
| 产品描述 | Ricolinostat is an orally bioavailable, specific inhibitor of histone deacetylase 6 (HDAC6) with potential antineoplastic activity. |
| 靶点活性 | HDAC6:4.7 nM, HDAC8:100 nM, HDAC1:58 nM, HDAC3:51 nM, HDAC2:48 nM |
| 体外活性 | 在浆细胞瘤模型和弥散性MM模型中,ACY-1215易被肿瘤组织吸收并且不会在组织中积累,能够抑制肿瘤生长. |
| 体内活性 | 在极低剂量时,ACY-1215能够显著诱导α-tubulin乙酰化,同时在较高剂量时,能够诱导组蛋白H3和H4组蛋白赖氨酸的乙酰化。在HDAC4, HDAC5, HDAC7, HDAC9, HDAC11, Sirtuin1,和 Sirtuin2,对HDAC8中,ACY-1215,ACY-1215(IC50=0.1 μM) 有轻微的活性。 |
| 激酶实验 | ACY-1215 is dissolved and subsequently diluted in assay buffer [50 mM HEPES, pH 7.4, 100 mM KCl, 0.001% Tween-20, 0.05% BSA, and 20 μM tris(2-carboxyethyl)phosphine] to 6-fold the final concentration. HDAC enzymes are diluted to 1.5-fold of the final concentration in assay buffer and pre-incubated with ACY-1215 for 10 minutes before the addition of the substrate. The amount of FTS (HDAC1, HDAC2, HDAC3, and HDAC6) or MAZ-1675 (HDAC4, HDAC5, HDAC7, HDAC8, and HDAC9) used for each enzyme is equal to the Michaelis constant (Km), as determined by a titration curve. FTS or MAZ-1675 is diluted in assay buffer to 6-fold the final concentration with 0.3 μM sequencing grade trypsin. The substrate/trypsin mix is added to the enzyme/compound mix and the plate is shaken for 60 seconds and then placed into a SpectraMax M5 microtiter plate reader. The enzymatic reaction is monitored for release of 7-amino-4-methoxy-coumarin over 30 minutes, after deacetylation of the lysine side chain in the peptide substrate, and the linear rate of the reaction is calculated[1]. |
| 细胞实验 | ACY-1215 is dissolved in DMSO (10 mM) and stored, and then in diluted with appropriate culture medium before use[1]. The effect of ACY-1215 with or without Bortezomib on the viability of MM cell lines, patient MM cells, and PBMCs is assessed by measuring MTT dye absorbance. PBMCs from healthy donors are isolated and stimulated with 2.5 μg/mL of phytohemagglutinin (PHA) for 48 hours in the presence of increasing concentrations of ACY-1215. DNA synthesis is measured by tritiated thymidine uptake. CD4+ T cells are purified from human blood with the Rosette Sep negative-selection kit. Cells are stimulated by CD3/CD28 Dynabeads for 7 days in the presence of compounds. Cell viability is assessed using alamarBlue. MM cells (2-3×104 cells/well) are incubated in 96-well culture plates with medium and different concentrations of ACY-1215, Bortezomib, and/or recombinant IL-6 (10 ng/mL) or insulin-like growth factor-1 (IGF-1; 50 ng/mL) for 24 hours at 37°C, and tritiated thymidine incorporation is measured[1]. |
| 别名 | ACY-1215, Rocilinostat |
| 分子量 | 433.5 |
| 分子式 | C24H27N5O3 |
| CAS No. | 1316214-52-4 |
存储
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
Ethanol: <1 mg/mL
DMSO: 80 mg/mL (184.5 mM)
( < 1 mg/mL refers to the product slightly soluble or insoluble )
联系我们：
邮箱：2519696869@qq.com
QQ: 2519696869
电话：18066853083
微信：18066853083
公司介绍：
西安齐岳生物科技有限公司是集化学科研和定制与一体的高科技化学公司。业务范围包括化学试剂和产品的研发、生产、销售等。涉及产品为通用试剂的分销、非通用试剂的定制与研发，涵盖生物科技、化学品、中间体和化工材料等领域。
主营产品：COF、MOF单体系列：三蝶烯衍生物、金刚烷衍生物、四苯甲烷衍生物、peg、上转换、石墨烯、光电材料、点击化学、凝集素、载玻片、蛋白质交联剂、脂质体、蛋白、多肽、氨基酸、糖化学等。
