ik 1

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.

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

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]

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.

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.

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.

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].

Chromanol 293B is an inhibitor of the slow component (IK) of delayed rectifier potassium currents in cardiac cells (IC50 = 1–10 μM) and a weak inhibitor of KATP channels. It also blocks CFTR chloride currents (IC50 = 19 μM) and can be used in arrhythmia research.

NS309 is a nonselective activator of small- and intermediate-conductance Ca2+-activated K+ (SK/KCa2 and IK/KCa3.1) channels (EC50s range from 0.12-1.2 µM for SK channels and 10-90 nM for IK channels). It can also activate voltage-gated Kv11.1 channels (hE