SIKs-IN-1

SIKs-IN-1 (compound 8h), a pyrimidine-5-carboxamide derivative, is a Salt-inducible kinases (SIKs) inhibitor. SIKs regulates the transformation of M1/M2 macrophages, involving in inflammation process. SIKs-IN-1 inhibits SIK activity, up-regulates anti-inflammatory cytokine IL-10, but down-regulates pro-inflammatory cytokine IL-12. SIKs-IN-1 shows excellent anti-inflammatory effects in a DSS-induced colitis model[1].

Product Specifications

CAS Number

[2927557-06-8]

UNSPSC

12352005

Target

Salt-inducible Kinase (SIK)

Type

Reference compound

Related Pathways

Immunology/Inflammation

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/siks-in-1.html

Solubility

10 mM in DMSO

Smiles

O=C(NC1=C(F)C=CC=C1C)C2=C(NC3CCC3)N=C(NC4=CC=C(N5CCN(C)CC5)C(F)=C4)N=C2

Molecular Formula

C27H31F2N7O

Molecular Weight

507.58

References & Citations

[1]Cai X, et al. Discovery of pyrimidine-5-carboxamide derivatives as novel salt-inducible kinases (SIKs) inhibitors for inflammatory bowel disease (IBD) treatment. Eur J Med Chem. 2023 Aug 5;256:115469.