sk1

PF-543 (Sphingosine Kinase 1 Inhibitor II), a novel sphingosine-competitive inhibitor of SphK1, inhibits SphK1 with IC50 of 2.0 nM and Ki of 3.6 nM.

PF-543 hydrochloride (PF-543) inhibits SphK1 with a K(i) of 3.6 nM, is sphingosine-competitive and is more than 100-fold selective for SphK1 over the SphK2 isoform.

SK1-IN-1 is an orally available and potent sphingosine kinase 1 (SPHK1) inhibitor (IC50: 58 nM), with potential anticancer activity, and can be used to study cancer and neurodegenerative diseases.

BML-258 HCl was removed and discontinued.

SK1-I hydrochloride is the salt form of SK1-I(BML-258). SK1-I is a selective and competitive sphingosine kinase 1 (SphK1) inhibitor and sphingosine analog that is inactive against SphK2 and a variety of other protein kinases, and possesses anti-leukemic potential to inhibit tumor cell growth and promote apoptosis.

SSK1 is a compound that selectively kills senescent cells and is a precursor for β-galactosidase, which can reduce the inflammatory response of the body. SSK1 can activate the phosphorylation of p38 MAPK and MKK3/MKK6 in senescent cells, and promote mitochondrial DNA damage in senescent cells.

GSK1940029 (SCD inhibitor 1) is an inhibitor of stearoyl-CoA desaturase (SCD).

GSK1904529A (GSK 4529) is a specific inhibitor of IGF-1R (IC50=27 nM) and IR(IC50=25 nM) .

HSK16149 is a novel ligand of voltage-gated calcium channel (VGCC) α 2 δ subunit with analgesic activity.

GSK1016790A (GSK101) (GSK101) is a novel, potent activator of TRPV4 (transient receptor potential vanilloid 4) with EC50 of 34 nM in choroid plexus epithelial cells.

ASK1-IN-4 is an ASK1 inhibitor, IC50 = 0.2 μM.

GSK199 is a selective PAD4 inhibitor(IC50 of 200 nM in the absence of calcium).

ASK1-IN-1 is an inhibitor of apoptosis signal-regulating kinase 1 which is a key mediator in the apoptotic and inflammatory cellular stress response with an IC50 of 21 nM in biochemica assays.

GSK1059865 is a potent antagonist of the orexin 1 receptor.

GSK1521498 free base (hydrochloride) is a selective μ-opioid receptor (MOR) antagonist used to treat compulsive consumption disorders involving food, alcohol, and drugs.

GSK1521498 free base is an effective and selective μ-opioid receptor antagonist with potential applications in obesity, alcoholism, and drug addiction.

GSK1521498 is a selective antagonist of the μ-opioid receptor (MOR). It is being used for the treatment of disorders of compulsive consumption of food, alcohol, and drugs.

GSK1379725A is a selective BPTF ligand [Kd = 2.8 μM].

GSK1702934A, a selective TRPC3 agonist, modulates cardiac contractility and arrhythmogenesis through TRPC3 activation.

GSK180 is a selective competitive inhibitor of kynurenine 3-monooxygenase (KMO; IC50: ~6 nM), an enzyme involved in tryptophan metabolism.

GSK163929 (compound 122) is an orally active CCR5 antagonist with anti-HIV properties and demonstrates low inhibitory potency against hEGR. Administered at a dosage of 2000 mg kg day (i.v., 7 d), it shows no adverse effects in rats, and at 250 mg kg day (i.v., 7 d), it is similarly non-toxic in dogs.

ASK1-IN-7 (Compound 4c) is an ASK1 inhibitor and a derivative of the ASK1 inhibitor scaffold 5-(5-Phenyl-furan-2-ylmethylene)-2-thioxo-thiazolidin-4-one. This compound is potentially applicable in research involving ASK1 signaling pathways, including studies on cellular stress response, inflammatory response, neurodegenerative diseases, and cardiovascular diseases.

ASK1-IN-8 (Compound 35) is an orally active inhibitor of apoptosis signal-regulating kinase 1 (ASK1) with an IC50 value of 1.8 nM. In a mouse liver injury model induced by Acetaminophen, ASK1-IN-8 significantly reduces plasma alanine aminotransferase (ALT) levels, offering liver protection. This compound is useful for research in liver disease-related fields.

GSK126 (GSK2816126A) is a excellently specific EZH2 methyltransferase inhibitor ( IC50=9.9 nM).