上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。
HDAC/Top-IN-1
HDAC/Top-IN-1 是一种具有口服活性的、广谱的 HDAC/Top 双重抑制剂，对 HDAC1、HDAC2、HDAC3、HDAC6 和 HDAC8 的 IC50 分别为 0.036 μM、0.14 μM、0.059 μM、0.089 μM 和 9.8 μM。HDAC/Top-IN-1 能有效诱导 HEL 细胞凋亡 (apoptosis)，能将细胞阻滞在 S 期。
HDAC/Top-IN-1 Chemical Structure
CAS No. : 2411379-14-9
| 规格 |
|
是否有货 |
|
| 100 mg |
|
询价 |
|
| 250 mg |
|
询价 |
|
| 500 mg |
|
询价 |
|
* Please select Quantity before adding items.
| 生物活性 |
HDAC/Top-IN-1 is an orally active and pan HDAC/Top dual inhibitor with IC50s of 0.036 μM, 0.14 μM, 0.059 μM, 0.089 μM and 9.8 μM for HDAC1, HDAC2, HDAC3, HDAC6 and HDAC8. HDAC/Top-IN-1 efficiently induces apoptosis with S cell-cycle arrest in HEL cells. HDAC/Top-IN-1 has exhibits excellent in vivo antitumor efficacy[1].
|
| IC50 & Target[1] |
|
HDAC1
34 nM (IC50)
|
HDAC2
140 nM (IC50)
|
HDAC3
59 nM (IC50)
|
HDAC6
89 nM (IC50)
|
HDAC8
9.8 μM (IC50)
|
|
体外研究
(In Vitro) |
HDAC/Top-IN-1 (compound 16j) (0-2 μM; 48 hours) exhibits remarkable inhibitory activities against the tested cell lines[1].
HDAC/Top-IN-1 (20 and 100 nM; 24 hours) dramatically increases acetyl-H3 and acetyl-H4 levels in HEL cells[1].
HDAC/Top-IN-1 (0.1 and 0.5 μM; 48 hours) effectively induces HEL cell apoptosis in a dose-dependent manner[1].
HDAC/Top-IN-1 (0.02-0.5 μM; 48 hours) arrests HEL cells at the S phase[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Proliferation Assay
| Cell Line: |
MCF-7, A549, HCT116, HepG-2, K562 and HEL[1] |
| Concentration: |
0-2 μM |
| Incubation Time: |
48 hours |
| Result: |
Exhibited remarkable inhibitory activities against the tested cell lines, and IC50s of 0.68, 0.21, 0.26, 0.35 and 0.029 μM in MCF-7, A549, HCT116, HepG-2, K562 and HEL, respectively. |
Western Blot Analysis
| Cell Line: |
HEL[1] |
| Concentration: |
20 and 100 nM |
| Incubation Time: |
24 hours |
| Result: |
Dramatically increased in acetyl-H3 and acetyl-H4 levels. |
Apoptosis Analysis
| Cell Line: |
HEL[1] |
| Concentration: |
0.1 and 0.5 μM |
| Incubation Time: |
48 hours |
| Result: |
Led to 56.02% and 76.45% apoptotic cell death at concentration of 0.1 and 0.5 μM, respectively |
Cell Cycle Analysis
| Cell Line: |
HEL[1] |
| Concentration: |
0.02, 0.1 and 0.5 μM |
| Incubation Time: |
48 hours |
| Result: |
The ratios in the S phase were changed dramatically 9.8%, 15.4%, and 25.8% at 0.02, 0.1 and 0.5 μM, respectively. |
|
体内研究
(In Vivo) |
HDAC/Top-IN-1 exhibits good metabolic properties with a half-life (T1/2) of 31.49 min, and the clearance is 173.32 mL/min/mg[1].
HDAC/Top-IN-1 (5 and 10 mg/kg; PO; daily, for 14 days) exhibits potent oral antitumor activity[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: |
Female BALB/C nude mice (5-6 weeks, 18-20 g; injected with human K562 cells)[1] |
| Dosage: |
5 and 10 mg/kg |
| Administration: |
PO; daily, for 14 days |
| Result: |
Exhibited potent oral antitumor activity at 5 mg/kg with a TGI value of 41.4% and a T/C value of 54.3%, and achieved better tumor growth inhibition with a TGI of 68.5% and a T/C of 25.5%. |
|
| 分子量 |
|
| Formula |
|
| CAS 号 |
|
| 运输条件 |
Room temperature in continental US; may vary elsewhere.
|
| 储存方式 |
Please store the product under the recommended conditions in the Certificate of Analysis.
|
| 参考文献 |
-
[1]. Wu S, Huang Y, Wang T, et al. Evodiamine-Inspired Topoisomerase-Histone Deacetylase Dual Inhibitors: Novel Orally Active Antitumor Agents for Leukemia Therapy. J Med Chem. 2022;65(6):4818-4831.
|
所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务
