您好,欢迎来到化工原料网! [登录] [免费注册]
化工原料网
位置:首页 > 产品库 > UNC0379 TFA
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:
 
UNC0379 TFA
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。
UNC0379 TFA图片
CAS NO:1620401-83-3
包装与价格:
包装价格(元)
2mg电议
5mg电议
10mg电议
50mg电议

产品介绍
UNC0379 TFA 是一个选择性的底物竞争性的赖氨酸甲基转移酶SETD8(KMT5A) 抑制剂,IC50值为 7.3 μM,KD值 of 18.3 μM。UNC0379 TFA 可用于炎症癌症的研究,如肺纤维化,卵巢癌,神经母细胞瘤。
生物活性

UNC0379 TFA is a selective, substrate-competitive inhibitor oflysine methyltransferase SETD8(KMT5A) with anIC50of 7.3 μM,KDvalue of 18.3 μM. UNC0379 TFA can be used in the research of inflammation and cancers, such as pulmonary fibrosis, ovariancancer, neuroblastoma[1][2][3].

IC50& Target

SETD8 (KMT5A)[1]

体外研究
(In Vitro)

UNC0379 TFA (1-10 μM, 9 days) inhibits HGSOC cells proliferation[2].
UNC0379 TFA (10 μM, 96 h) increases in the proportion of sub-G1 phase cells in HGSOC cells[2].
UNC0379 TFA (10 μM, 48 h) induces myofibroblast de-differentiation and inhibits additional fibroblast to myofibroblast differentiation[3].

Cell Viability Assay[1]

Cell Line:JHOS2, JHOS3, JHOS4, OVCAR3, OVCAHO, OVKATE, KURAMOCHI, TYKnu
Concentration:1-10 μM
Incubation Time:9 days
Result:Inhibited HGSOC cells proliferation withIC50s ranging from 0.39 to 3.20 μM.

Cell Cycle Analysis[1]

Cell Line:JHOS3, OVCAR3
Concentration:10 μM
Incubation Time:96 h
Result:Arrested cells in sub-G1 phase.
体内研究
(In Vivo)

UNC0379 TFA (intratracheal administration, 1 mg/kg/day, 1 mg/kg/day, on day7, 8, and 9) ameliorates the lung fibrosis in Bleomycin (BLM)-induced lung fibrosis mouse[3].

Animal Model:Bleomycin (BLM)-induced lung fibrosis mouse model[3]
Dosage:1 mg/kg/day
Administration:Intratracheal administration, on day7, 8, and 9.
Result:Ameliorated BLM-induced lung fibrosis (supported by the evaluation of the Ashcroft score and changes in the collagen content in the lung samples) without affecting pulmonary inflammation.
分子量

527.58

性状

Solid

Formula

C25H36F3N5O4

CAS 号

1620401-83-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

H2O : 100 mg/mL(189.54 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM1.8954 mL9.4772 mL18.9545 mL
5 mM0.3791 mL1.8954 mL3.7909 mL
10 mM0.1895 mL0.9477 mL1.8954 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。