SIK

RSS0680 is a protein kinase degrader that degrades a variety of kinases and can be used to study diseases caused by kinase abnormalities.

WH-4-025 is a Salt-inducible kinase (SIK) inhibitor that targets the SIK family of proteins.

Prexasertib (LY2606368) is a selective checkpoint kinase 1 (CHK1) inhibitor (Ki 0.9 nM, IC50<1 nM). Prexasertib causes double-stranded DNA breaks and replication mutations, leading to apoptosis. Prexasertib has antitumor activity.

Prexasertib dihydrochloride (LY2606368) is an ATP-competitive CHK1 inhibitor (Ki: 0.9 nmol/L). in the cell-free assay, its IC50 values are 8 nM and 9 nM for CHK2 and RSK, respectively.

GSK-1070916 (GSK-1070916A) is a reversible and ATP-competitive inhibitor of Aurora B/C with IC50 of 3.5 nM/6.5 nM. It displays >100-fold selectivity against the closely related Aurora A-TPX2 complex. Phase 1.

SIK-IN-4 (compound 34) acts as a potent inhibitor of SIK, exhibiting IC 50 values of 1.2 nM for SIK1, 0.9 nM for SIK2, and 1.8 nM for SIK3.

SIK-IN-3 (Compound 6B) is an inhibitor of salt-induced kinases (SIK), demonstrating inhibitory effects on SIK1, SIK2, and SIK3 with IC50 values of 0.1, 0.3, and 0.8 nM respectively. SIK-IN-1 inhibits TNFa release in human macrophages with an IC50 of 0.6 nM and stimulates LPS-induced IL-10 release with an EC50 of 3 nM.

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].

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].

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].

SIK2/3-IN-1 (Compound 7S) is an orally active and selective inhibitor of SIK2/3. It significantly inhibits tumor growth without causing weight loss in the MV4-11 AML mouse CDX model. SIK2/3-IN-1 is applicable for research in MEF2C-dependent acute myeloid leukemia.

SIK2-IN-3 is an orally active selective inhibitor of SIK1/2 with IC50 values of 0.128/0.084 μM. It hinders the phosphorylation of CRTC3 and suppresses the production of pro-inflammatory factors in myeloid cells. Additionally, SIK2-IN-3 alleviates systemic and tissue inflammatory responses in a mouse anti-CD40 colitis model.

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.

SIK1 activator 1 can enhances the SIK1 phosphorylation and ameliorated the hyperglyceamia of type 2 diabetic mice. SIK1 activator 1 exhibited remarkable inhibitory activity on hepatic gluconeogenesis.

SIK2-IN-1 (compound 8g) is a potent and selective inhibitor of SIK2 over other AMPK-family kinases, exhibiting favorable ADMET profiles in vitro and robust cellular activities [1].

Sikokianin E, a biflavonone derivative, is isolable from Coreopsis tinctoria [1].

Sikokianin C is a biflavonoid isolated from Wikstroemia sikokiana.Sikokianin C is a selective cystathionine β-synthase inhibitor with antitumour activity for the treatment of human colon cancer.

Campsiketalin is a natural product for research related to life sciences. The catalog number is TN5830 and the CAS number is 93675-96-8.

Sikokianin A shows in vitro antiviral activity against HBsAg secretion.

MRT199665 is an effective and ATP-competitive, selective MARK/SIK/AMPK inhibitor (IC50s of 2/2/3/2 nM, 10/10 nM, and 110/12/43 nM for MARK1/MARK2/MARK3/MARK14, AMPKα1/AMPKα2, and SIK1/SIK2/SIK3, respectively). MRT199665 suppresses the phosphorylation of S

YKL-06-062 is a second-generation salt-inducible kinase (SIK) inhibitor that targets SIK1, SIK2, and SIK3, with IC50 values of 2.12 nM, 1.40 nM, and 2.86 nM, respectively.

MRT 67307 dihydrochloride is a dual inhibitor of the IKKε and TBK-1 with IC50s of 160 and 19 nM, respectively. MRT67307 dihydrochloride also inhibits ULK1 and ULK2 with IC50s of 45 and 38 nM, respectively. MRT67307 dihydrochloride also blocks autophagy in cells.

GLPG3970 GLPG3970 is a novel orally available selective dual SIK2/SIK3 inhibitor.GLPG3970 has potential anti-inflammatory activity for the study of autoimmune diseases.

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]