ik1

IK1 inhibitor PA-6 (PA-6) is a selective and potent inhibitor of IK1 (KIR2.x ion-channel-carried inward rectifier current) with an IC50 of 12-15 nM for human and mouse KIR2.x currents.

Zacopride is a highly potent 5-HT3 receptor antagonist (Kd = 0.38 nM) and 5-HT4 receptor agonist (Ki = 373 nM). It also is a selective IK1 channel agonist.

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-IN-1 (Compound 27) is a selective inhibitor of salt-inducible kinase 1 (SIK1) with an IC50 of 0.7 nM, demonstrating greater potency for SIK1 compared to SIK2 and SIK3. It shows no cytotoxicity in HEK293 cells and PBMC at concentrations up to 30 μM. Additionally, SIK1-IN-1 effectively inhibits 392 kinases, particularly tyrosine kinases such as FGR, HCK, and LYN.

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.

IBMX (Methylisobutylxanthine) is a broad-spectrum phosphodiesterase (PDE) inhibitor with inhibitory activity against PDE3, PDE4, and PDE5 (IC50=6.5/26.3/31.7 μM). IBMX enhances the intracellular cAMP level.

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.

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

C 101248 (KCNK13-IN-1) is a selective and potent tandem pore halogen inhibitor of K+ channel 1 (THIK-1) inhibitor and human and mouse KCNK13 inhibitor.C 101248 inhibits IL-1β release in a concentration-dependent manner and can be used for the study of inflammation induced by neurodegenerative disorders.

PF-07899895 (compound 34) is a potent SIK (salt-induced kinase) inhibitor with IC50 values of 1.2/0.9/1.8 nM for SIK1/SIK2/SIK3.

TWIK-1/TREK-1-IN-3 is a selective and potent inhibitor of the potassium channel TREK-1, effectively inhibiting TREK-1 homodimers and TWIK-1/TREK-1 heterodimers containing two-pore-domain potassium (K2p) channels. TWIK-1/TREK-1-IN-3 exhibits antidepressant activity and can be utilized in the study of depression.

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]

CLIK-148 is an oral, highly selective, irreversible inhibitor of cysteine protease that primarily targets cathepsin L. It effectively impedes the cathepsin L-dependent degradation of HMG-CoA reductase on the endoplasmic reticulum (ER) membrane. Additionally, CLIK-148 inhibits the cathepsin L-mediated processing of procholecystokinin (proCCK), leading to reduced production of CCK8. By obstructing cathepsin L degradation of type I collagen secreted by osteoclasts, CLIK-148 decreases tumor-induced bone metastasis and malignant hypercalcemia. This compound is valuable for research into bone metabolism disorders and neuropeptide processing regulation.

A1899 is a effective and selective TASK-1 and TASK-3 antagonist.

PIK-108 is an allosteric inhibitor of phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunits β and δ (PI3Kβ/δ).

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-06-061 is a selective salt-inducible kinase (SIK) inhibitor with IC50 values of 6.56 nM/1.77 nM/20.5 nM for SIK1/2/3, respectively.

ARN-3236 is an orally active and selective inhibitor of salt-inducible kinase 2 (SIK2), with IC50 values of <1 nM for SIK2, 21.63 nM for SIK1, and 6.63 nM for SIK3. ARN-3236 exhibits anti-cancer activity.

PIK-124 is a potent PI3K inhibitor.

NIK-12192 is an indole derivative and inhibitor of vacuolar-H(+)-ATPase.

Compound 2a, identified as TWIK-1/TREK-1-IN-1, acts as an inhibitor of the TREK-1, a two-pore domain potassium channel (K2p) that forms TREK-1 homodimers and TWIK-1/TREK-1 heterodimers, both significant for its role as an antidepressant target. Furthermore, TWIK-1/TREK-1-IN-3, a related compound, selectively inhibits these channels with IC50 values of 9.36 μM for TREK-1 homodimers and 14.6 μM for TWIK-1/TREK-1 heterodimers, demonstrating antidepressant-like effects [1].

TWIK-1/TREK-1-IN-2 (Compound 2g) serves as an inhibitor of both TWIK-1 and TREK-1, targeting the TREK-1 homodimer and TWIK-1/TREK-1 heterodimer with IC50 values of 10.13 μM and 15.5 μM, respectively; additionally, it exhibits antidepressant properties [1].

IEIK 13, a self-assembling peptide (SAP), is employed in cartilage tissue engineering research [1].