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Merck
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重要文件

SML0744

Sigma-Aldrich

LDN-27219

≥98% (HPLC)

同義詞:

2-[(3,4-Dihydro-4-oxo-3,5-diphenylthieno[2,3-d]pyrimidin-2-yl)thio]-acetic acid hydrazide

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About This Item

經驗公式(希爾表示法):
C20H16N4O2S2
CAS號碼:
分子量::
408.50
分類程式碼代碼:
12352200
NACRES:
NA.77
暫時無法取得訂價和供貨情況

化驗

≥98% (HPLC)

形狀

powder

顏色

white to beige

溶解度

DMSO: 15 mg/mL, clear

儲存溫度

−20°C

SMILES 字串

[s]1c2nc([n]([c](c2c(c1)c4ccccc4)=O)c3ccccc3)SCC(=O)NN

InChI

1S/C20H16N4O2S2/c21-23-16(25)12-28-20-22-18-17(15(11-27-18)13-7-3-1-4-8-13)19(26)24(20)14-9-5-2-6-10-14/h1-11H,12,21H2,(H,23,25)

InChI 密鑰

WLBUICQBNZXIDJ-UHFFFAOYSA-N

生化/生理作用

LDN-27219 is a revesible inhibitor of transglutaminase 2 (TG2) that binds to the GTP binidng site of the enzyme and inhbits activity with and IC50 of 600 nM.
LDN-27219 is a revesible inhibitor of transglutaminase 2 (TG2).
LDN-27219 is a thieno[2,3-d]pyrimidine-4-one-acylhydrazide derivative.[1] Closed conformation of TG2 induced by LDN-27219 can be a potential therapeutic strategy for age-related vascular dysfunction and lowering blood pressure.[2]

象形圖

Exclamation mark

訊號詞

Warning

危險聲明

危險分類

Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3

標靶器官

Respiratory system

儲存類別代碼

11 - Combustible Solids

水污染物質分類(WGK)

WGK 3

閃點(°F)

Not applicable

閃點(°C)

Not applicable


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分析證明 (COA)

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Nayeon Kim et al.
Organic & biomolecular chemistry, 12(27), 4932-4940 (2014-06-01)
In the process of optimization, we developed a novel core skeleton of thieno[3,4-b]pyrazine via GK-13. The derivatives synthesized were shown to inhibit TGase 2 activity in cancer cells. Some of the hit compounds such as the arylethynyl group-coupled thieno[3,4-b]pyrazine derivatives
Estéfano Pinilla et al.
Hypertension (Dallas, Tex. : 1979), 77(1), 216-227 (2020-12-01)
Transglutaminase 2 (TG2) is an enzyme which in the open conformation exerts transamidase activity, leading to protein cross-linking and fibrosis. In the closed conformation, TG2 participates in transmembrane signaling as a G protein. The unspecific transglutaminase inhibitor cystamine causes vasorelaxation

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