1. Protein Tyrosine Kinase/RTK
  2. Syk
  3. MRL-SYKi

MRL-SYKi 是一种对脾酪氨酸激酶(SYK)具有高选择性和强效活性的化学探针。MRL-SYKi 在完整活细胞中强效结合 SYK 功能增 (GoF) 变体 (SYK(S550Y)、SYK(S550F) 和 SYK(P342T)),在二吉托宁透化的细胞实验中,IC50 值分别为 2.1 nM、14 nM 和 4.6 nM。MRL-SYKi 有效降低催化活性,在 PhosphoSens SOX 肽实验中,SYK(S550F) 的 IC50 = 63 nM,SYK(P342T) 的 IC50 = 95 nM。MRL-SYKi 可降低 SW480 细胞中 SYK(S550Y) 在 Y525/526 位的磷酸化水平。MRL-SYKi 可用于炎症研究。

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MRL-SYKi

MRL-SYKi Chemical Structure

CAS No. : 1312534-69-2

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  • 生物活性

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生物活性

MRL-SYKi is a chemical probe with high selectivity and potent activity against spleen tyrosine kinase (SYK). MRL-SYKi potently binds to SYK gain-of-function (GoF) variants (SYK(S550Y), SYK(S550F), and SYK(P342T)) in intact live cells, with IC50 values of 2.1 nM, 14 nM, and 4.6 nM respectively in digitonin-permeabilized cell assays. MRL-SYKi effectively reduces catalytic activity (IC50 = 63 nM for SYK(S550F) and 95 nM for SYK(P342T) in PhosphoSens SOX peptide assays). MRL-SYKi can decrease the phosphorylation level of SYK(S550Y) at Y525/526 in SW480 cells. MRL-SYKi can be used for the study of inflammation[1].

分子量

452.57

Formula

C24H28N4O3S

CAS 号
性状

固体

颜色

Off-white to light yellow

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
纯度 & 产品资料
参考文献
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
MRL-SYKi
目录号:
HY-178129
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