您好,欢迎来到试剂信息网! [登录] [免费注册]
试剂信息网
位置:首页 > 产品库 > NN-390
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
NN-390
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
NN-390图片
CAS NO:2490284-25-6
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
NN-390 是一种有效的选择性HDAC6抑制剂,其IC50为 9.8 nM。NN-390 可穿透血脑屏障。NN-390 在转移性第 3 组成神经管细胞瘤中显示出研究潜力。
生物活性

NN-390 is a potent and selectiveHDAC6inhibitor, with anIC50of 9.8 nM. NN-390 penetrates the blood-brain barrier (BBB). NN-390 shows study potential in metastatic Group 3 MB (medulloblastoma)[1].

IC50& TargetHDAC

HDAC2

>5 μM (IC50)

HDAC1

>5 μM (IC50)

HDAC6

9.8 nM (IC50)

HDAC3

>1 μM (IC50)

HDAC8

>1 μM (IC50)

HDAC11

>1 μM (IC50)

体外研究
(In Vitro)

NN-390 exhibits cellular potency withIC50values of 1.19 μM in MV4-11 cells and 1.38 μM in MM.1S cells while having minimal effects on noncancerous counterparts (IC50>50 μM in MRC-9)[1].
NN-390 (72 h) strongly decreases proliferation in HD-MB03 cells, with anIC50of 0.13 μM, and significantly impairs self-renewal of BTIC-enriched HD-MB03s[1].
NN-390 (0-2 μM, 1 h) markedly increases acetylation of α-tubulin and minimally changes acetylated histone H3[1].
NN-390 (6 h) results in acetylation of α-tubulin from concentrations as low as 0.1 μM (0-0.2 μM), and dose-dependent increases in acetylation of α-tubulin (0-0.2 μM)[1].
NN-390 (0-2 μM, 24 h) promotes cancer cells apoptosis in MV4-11 cells[1].

Immunofluorescence

Cell Line:HeLa cells[1]
Concentration:0, 0.1, 0.25, 1, 2 μM
Incubation Time:1 h
Result:Markedly increased acetylation of α-tubulin and minimally changed acetylated histone H3.

Western Blot Analysis

Cell Line:AML (MV4-11) cells[1]
Concentration:0, 0.1, 0.5, 1, 5 μM
Incubation Time:6 h
Result:Resulted in acetylation of α-tubulin from concentrations as low as 0.1 μM and with limited acetylation of histone H3 at only the highest concentration of 5 μM.

Western Blot Analysis

Cell Line:Group 3 MB (HD-MB03) cells[1]
Concentration:0, 0.053, 0.106, 0.158, 0.211 μM
Incubation Time:6 h
Result:Dose-dependent increased in acetylation of α-tubulin from the lowest concentration of 53 nM, with no observable change in acetylation of off-target histone H3 up to 211 nM.

Apoptosis Analysis

Cell Line:MV4-11 cells[1]
Concentration:0, 0.25, 0.75, 1, 2 μM
Incubation Time:24 h
Result:Promoted cancer cells apoptosis, 39% of cancer cells were undergoing late-stage apoptosis after 18 h at 2 μM, and 11% of cells were in the late apoptosis stage at 0.25 μM.
体内研究
(In Vivo)

NN-390 (male CD-1 mice, 20 mg/kg, IP, single dose) increases plasma stability[1].
NN-390 can improve PAMPA (parallel artificial membrane permeability assay)-BBB (blood-brain barrier) score[1].
Pharmacokinetic Parameters of NN-390 in male male CD-1 mice[1].

CompoundKT-5315a; NN-390
t1/2(h)1.051.90
Cmax(ng/mL)493750
AUClast(h*ng/mL)15762523
AUClnf(h*ng/mL)15192548
AUC/D (h*ng/mL)79126

Animal Model:CD-1 mice (male, n=3)[1]
Dosage:20 mg/kg
Administration:IP, single dose (Pharmacokinetic Analysis)
Result:Had a half-life of 115 min in human plasma, a 2.8-fold increase in stability.
分子量

420.38

Formula

C17H16F4N2O4S

CAS 号

2490284-25-6

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.