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

MRL-SYKi is a chemical probe for gain-of-function variants of spleen tyrosine kinase (SYK). MRL-SYKi reduces the catalytic activity of SYKS550Y, SYKS550F and SYKP342T, and downregulates the phosphorylation level of SYKS550Y. MRL-SYKi serves as a template for developing NanoBRET tracers targeting SYK, enabling NanoBRET cellular target engagement assays for gain-of-function variants of SYK. MRL-SYKi is applicable to research related to inflammatory and immune diseases.

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MRL-SYKi

MRL-SYKi Chemical Structure

CAS No. : 1312534-69-2

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Based on 1 publication(s) in Google Scholar

MRL-SYKi Related Antibodies

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Description

MRL-SYKi is a chemical probe for gain-of-function variants of spleen tyrosine kinase (SYK). MRL-SYKi reduces the catalytic activity of SYKS550Y, SYKS550F and SYKP342T, and downregulates the phosphorylation level of SYKS550Y. MRL-SYKi serves as a template for developing NanoBRET tracers targeting SYK, enabling NanoBRET cellular target engagement assays for gain-of-function variants of SYK. MRL-SYKi is applicable to research related to inflammatory and immune diseases[1].

In Vitro

MRL-SYKi potently inhibits purified SYK protein in cell-free enzymatic assays, with an IC50 of 30 nM[1].
MRL-SYKi (20 μM) binds to all tested NL-tagged SYK variants in digitonin-permeabilized HEK293 cells, with the highest potency against SYKS550Y (IC50 = 2.1 nM) and the lowest potency against SYKM450I (IC50 = 29 nM)[1].
MRL-SYKi (1-10 μM; 2 h) directly binds to NL-tagged SYKS550Y, SYKS550F, and SYKP342T in intact living HEK293 cells, with the highest potency against SYKS550Y (IC50 = 65 nM) and the lowest potency against SYKP342T (IC50 = 410 nM)[1].
MRL-SYKi (1.75-30 μM; 30 min) binds to NL-tagged SYK (WT) in digitonin-permeabilized HEK293 cells and increases its thermal stability, with a maximum ΔTm of 3.5 °C at the concentration of 30 μM[1].
MRL-SYKi (30 min) potently inhibits the catalytic activity of purified SYKS550F (IC50 = 63 nM) and SYKP342T (IC50 = 95 nM) in cell-free kinase activity assays[1].
MRL-SYKi (100 nM-10 μM; 20 h) reduces the phosphorylation level of SYKS550Y at Y525/526 in SW480 cells stably expressing SYKS550Y[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

MRL-SYKi Related Antibodies

Western Blot Analysis[1]

Cell Line: SW480 colonic epithelial cells stably expressing SYK(S550Y)
Concentration: 100 nM, 10 μM
Incubation Time: 20 h
Result: Reduced pSYK(Y525/526) levels compared to untreated cells at 100 nM.
Reduced pSYK(Y525/526) levels compared to untreated cells at 10 μM, with a greater reduction observed than at 100 nM.
Molecular Weight

452.57

Formula

C24H28N4O3S
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O[C@@]1(C2=NC=C(C3=CC(NC4=NC=CC(C)=N4)=CC(C)=C3)S2)CC(C)([C@H](CC1)C(O)=O)C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Purity & Documentation
References
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MRL-SYKi Related Classifications

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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.

Keywords:

MRL-SYKi1312534-69-2SykSpleen tyrosine kinaseSYK(S550F)intestinal inflammationSYK(P342T)immune dysregulationHEK293 cellsorgan inflammationskin inflammationspleen tyrosine kinaseSYK(S550Y)SW480 cellsInhibitorinhibitorinhibit

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