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化驗
>98% (HPLC)
形狀
powder
顏色
red-brown
溶解度
DMSO: soluble 18 mg/mL
H2O: insoluble
儲存溫度
2-8°C
SMILES 字串
CN(N=O)c1ccc(O)c(O)c1
InChI
1S/C7H8N2O3/c1-9(8-12)5-2-3-6(10)7(11)4-5/h2-4,10-11H,1H3
InChI 密鑰
XAKAQCMEMMZUEO-UHFFFAOYSA-N
基因資訊
human ... PTPN1(5770)
應用
Methyl-3,4-dephostatin has been used as:
- an inhibitor for methyltransferases
- a kinase-related inhibitor for human transglutaminase
- a cysteine binding compound for screening its effect on C-terminal domain (CTD) of human immunodeficiency virus (HIV-1) capsid protein
生化/生理作用
Methyl-3,4-dephostatin is a tyrphostin-related compound isolated from Streptomyces MJ742-NF5 strain. It favors nerve growth factor-based neurite formation in pheochromocytoma PC12 cells. Being a stable analog of the nitrosoaniline dephostatin, it can mimic phosphotyrosine substrate for Tyrosyl-DNA phosphodiesterase I (TdpI).
Stable analog of dephostatin; selective protein tyrosine phosphatase 1B and SHPTP-1 inhibitor; does not inhibit CD45-associated phosphatases.
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
個人防護裝備
Eyeshields, Gloves, type N95 (US)
Ebselen, a small-molecule capsid inhibitor of HIV-1 replication
Antimicrobial Agents and Chemotherapy, 60(4), 2195-2208 (2016)
A high throughput scintillation proximity imaging assay for protein methyltransferases
Combinatorial Chemistry & High Throughput Screening, 15(5), 359-371 (2012)
Chemistry & biology, 15(9), 969-978 (2008-09-23)
Human tissue transglutaminase (TGM2) is a calcium-dependent crosslinking enzyme involved in the posttranslational modification of intra- and extracellular proteins and implicated in several neurodegenerative diseases. To find specific inhibitors to TGM2, two structurally diverse chemical libraries (LOPAC and Prestwick) were
Biochemical and biophysical research communications, 238(1), 213-217 (1997-09-23)
We studied the effect of the 3,4-dihydroxy analogue of dephostatin (3,4-dephostatin), an inhibitor of protein-tyrosine phosphatase (PTPase), on the differentiation of rat pheochromocytoma PC12 cells. 3,4-Dephostatin accelerated NGF-induced neurite formation in PC12h cells, a subline of PC12 cells, whereas the
The Journal of antibiotics, 48(12), 1460-1466 (1995-12-01)
We have synthesized derivatives of dephostatin, a protein tyrosine phosphatase (PTPase) inhibitor, to study the structure-activity relationships of this inhibitor. Inactive analogs revealed some insight into structural requirements or PTPase inhibitory activity of dephostatin. Both a nitroso group and phenolic
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