MRL-SYKi

• Description:

  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].

• UNSPSC:

  12352005

• Target:

  Syk

• Related Pathways:

  Protein Tyrosine Kinase/RTK

• Applications:

  COVID-19-immunoregulation

• Field of Research:

  Inflammation/Immunology

• Purity:

  99.9

• 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

• Molecular Formula:

  C24H28N4O3S

• Molecular Weight:

  452.57

• References & Citations:

  [1]Capener JL, et al. Development of SYK NanoBRET Cellular Target Engagement Assays for Gain-of-Function Variants. bioRxiv [Preprint]. 2024 Jun 13:2024.06.12.598544.

• Shipping Conditions:

  Room Temperature

• Storage Conditions:

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category:

  Reference compound1

• Clinical Information:

  No Development Reported

• CAS Number:

  [1312534-69-2]