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Merck
CN

SML1901

Sigma-Aldrich

ML348

≥98% (HPLC)

别名:

ML 348, ML-348, N- [2-氯-5-(三氟甲基)苯基] -2- [4-(2-呋喃基)-1-哌嗪基]乙酰胺

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About This Item

经验公式(希尔记法):
C18H17ClF3N3O3
分子量:
415.79
UNSPSC代码:
51111800
NACRES:
NA.77

质量水平

方案

≥98% (HPLC)

表单

powder

颜色

white to beige

溶解性

DMSO: 20 mg/mL, clear

储存温度

2-8°C

SMILES字符串

FC(F)(F)c1cc(c(cc1)Cl)NC(=O)CN2CCN(CC2)C(=O)c3[o]ccc3

InChI

1S/C18H17ClF3N3O3/c19-13-4-3-12(18(20,21)22)10-14(13)23-16(26)11-24-5-7-25(8-6-24)17(27)15-2-1-9-28-15/h1-4,9-10H,5-8,11H2,(H,23,26)

InChI key

OXKNHBBDOIMFFQ-UHFFFAOYSA-N

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生化/生理作用

ML348 是一种底物竞争性、可逆和 APT1 选择性酰基蛋白硫酯酶(APT)抑制剂(对 APT1 的 IC50/Ki = 840 nM/300 nM;对 APT2 的 IC50 & Ki >10 μM)。 ML348 可有效抑制培养物中(在 HEK293T & 小鼠 T 细胞中为 >95%;5 μM 持续 4 h)和小鼠体内(腹腔注射 50 mg/kg 后 4 小时,肺/心脏/肾脏中为 >90%,脑组织中约为 50%)的细胞 APT1 活性,而不会影响超过 15 种细胞丝氨酸水解酶和 APT2。

储存分类代码

11 - Combustible Solids

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable


历史批次信息供参考:

分析证书(COA)

Lot/Batch Number

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Alexander Adibekian et al.
Journal of the American Chemical Society, 134(25), 10345-10348 (2012-06-14)
The development of small-molecule inhibitors for perturbing enzyme function requires assays to confirm that the inhibitors interact with their enzymatic targets in vivo. Determining target engagement in vivo can be particularly challenging for poorly characterized enzymes that lack known biomarkers
Rahul S Kathayat et al.
Nature chemical biology, 13(2), 150-152 (2016-12-20)
Hundreds of human proteins are modified by reversible palmitoylation of cysteine residues (S-palmitoylation), but the regulation of depalmitoylation is poorly understood. Here, we develop 'depalmitoylation probes' (DPPs), small-molecule fluorophores, to monitor the endogenous activity levels of 'erasers' of S-palmitoylation, acylprotein
Jeannie L Hernandez et al.
Cell chemical biology, 24(1), 87-97 (2017-01-10)
The multidomain scaffolding protein Scribble (Scrib) organizes key signaling complexes to specify basolateral cell polarity and suppress aberrant growth. In many human cancers, genetically normal Scrib mislocalizes from cell-cell junctions to the cytosol, correlating with enhanced growth signaling and malignancy.

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