sik inhibitor-1

HG-9-91-01 (SIK inhibitor 1) is a potent and highly selective salt-inducible kinase (SIKs) inhibitor with IC50s of 0.92 nM, 6.6 nM and 9.6 nM for SIK1, SIK2 and SIK3respectively.

YKL-05-099 is a salt-inducible kinase (SIK) inhibitor. It can inhibit the activity of SIK1 (IC50: 10 nM) and SIK3 (IC50: 30 nM), and has a slightly weaker inhibitory effect on SIK2 (IC50: 40 nM). [1]

MRIA9, an ATP-competitive inhibitor targeting pan Salt-Inducible Kinases (SIK) and PAK2 3, demonstrates IC50 values of 516 nM, 180 nM, and 127 nM for SIK1, SIK2, and SIK3, respectively [1].

JRD-SIK1 2i-4 is a SIK1 2 inhibitor that induces nuclear translocation of CRTC3 at low micromolar concentrations. It is expected to saturate SIK1 and SIK2, but not SIK3.

SIK-IN-1 (Compound 53) acts as a potent inhibitor of salt-inducible kinase (SIK), specifically targeting SIK1, SIK2, and SIK3 with IC50 values of 0.1, 0.4, and 1.5 nM, respectively. Additionally, it effectively suppresses TNFa release with an IC50 of 0.5 nM and enhances LPS-induced IL-10 release in human macrophages with an EC50 of 4 nM [1].

SIKs-IN-1 (compound 8h), a pyrimidine-5-carboxamide derivative, functions as an inhibitor of Salt-inducible kinases (SIKs), which play a role in M1 M2 macrophage polarization linked to inflammation. By inhibiting SIK activity, this compound increases anti-inflammatory cytokine IL-10 and decreases pro-inflammatory cytokine IL-12, demonstrating significant anti-inflammatory efficacy in a DSS-induced colitis model [1].

SIK-IN-2 (Compound 45) is a potent inhibitor of salt-inducible kinase (SIK), effectively targeting SIK1, SIK2, and SIK3 with IC50 values of 0.1, 0.2, and 0.4 nM, respectively. Additionally, it suppresses TNFa release with an IC50 of 0.5 nM and promotes LPS-induced IL-10 release with an EC50 of 2 nM in human macrophages [1].